Iminosulfonylurea derivatives and herbicides

ABSTRACT

An iminosulfonylurea compound or a salt thereof which is useful as a herbicide and growth control agent against weeds.

This is a Division of application Ser. No. 08/170,222, filed on Apr. 15, 1994, now U.S. Pat. No. 5,500,466, which was filed as International Application No. PCT/JP92/00808, filed Jun. 25, 1992.

TECHNICAL FIELD

The present invention relates to novel iminosulfonylurea derivatives, and herbicides containing them as active ingredients.

BACKGROUND TECHNIQUE

It is indispensable to use herbicides to protect important crop plants such as rice, wheat, corn, soybean, cotton and sugar beet from weeds and thereby to increase the harvest. Especially in recent years, a selective herbicide is desired which is capable of selectively killing weeds without showing any phytotoxicity against crop plants when applied to the foliages of crop plants and weeds simultaneously in a field where such useful crop plants and weeds are coexistent. Further, with a view to avoiding environmental pollution and reducing the costs for transportation and application, researches and developments have been conducted for many years for compounds having high herbicidal effects at low doses. Some of the compounds having such properties are presently used as selective herbicides. However, there still exists a need for better new compounds having such properties.

As the prior art showing a chemical structure similar to that of the compounds of the present invention, Japanese Unexamined Patent Publications No. 15962/1983, No. 103371/1983, No. 126859/1983, No. 48973/1985, No. 214785/1985, No. 134377/1986, No. 151577/1989, No. 45473/1990, No. 91060/1990, No. 7284/1991 and No. 68562/1991, and U.S. Pat. Nos. 4,559,081, 4,592,776, 4,602,939, 4,622,065, 4,666,508, 4,696,695 and 4,741,762, disclose compounds having sulfonylurea bonded to a nitrogen atom. However, compounds having sulfonylurea bonded to a nitrogen atom of an imino structure like the compounds of the present invention have not been known at all, and they are novel compounds.

DISCLOSURE OF THE INVENTION

The present inventors have conducted extensive researches over years to develop selective herbicides for important crop plants and have studied herbicidal properties of many compounds with an aim to find out compounds having higher herbicidal activities as well as selectivity. As a result, it has been found that an iminosulfonylurea derivative of the formula (1) or an agriculturally suitable salt thereof: ##STR1## wherein Q is ##STR2## wherein in Q1, Q2 and Q5, E is a sulfur atom, an oxygen atom or a nitrogen atom mono-substituted by an optional substituent other than a hydrogen atom; in Q6, Q7 and Q8, J is a sulfur atom or an oxygen atom; in Q1 to Q8, a nitrogen atom in the ring of Q is substituted by an optional substituent other than a hydrogen atom, and a carbon atom in the ring of Q may be substituted by an optional substituent; and in Q9, the sulfur atom and the nitrogen atom on the carbon atom to which the imino group of Q is bonded, are substituted by optional substituents other than hydrogen atoms, Wherein Q is preferably ##STR3## R^(a1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(a2) and R^(a3) which are independent of each other, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(a4) and R^(a5) which are independent of each other, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(a6) is a C₂₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(b1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

R^(b2) is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(b3) is a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group,

R^(b4) is a hydrogen atom, or a C₁₋₆ alkyl group,

R^(b5) is a hydrogen atom, or a C₁₋₆ alkyl group,

R^(c1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(c2), R^(c3), R^(c4), R^(c5), R^(c6), R^(c11) and R^(c12) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(c7), R^(c8), R^(c9), R^(c10), R^(c13) and R^(c14) which are independent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(d2), R^(d3) and R^(d4) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d5) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d6) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(e1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₆ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(e2), R^(e3), R^(e6) and R^(e7) which are independent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(e4), R^(e5), R^(e8), R^(e9) and R^(e10) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(f1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

R^(f2) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(f3), R^(f4), R^(f7), R^(f8), R^(f11) and R^(f12) which are independent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(f5), R^(f6), R^(f9), R^(f10), R^(f13), R^(f14) and R^(f15) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(g1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(g2) and R^(g3) which are independent of each other, is a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group, a C₂₋₆ alkynyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkylsulfamoyl group, a di(C₁₋₃ alkyl)sulfamoyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a C₂₋₇ alkylcarbamoyl group, a di(C₁₋₃ alkyl)carbamoyl group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a benzyl group (provided that the phenyl group of such a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

or R^(g2) and R^(g3) form a saturated 3- to 7-membered heterocyclic ring together with the nitrogen atom to which they are bonded,

X is an oxygen atom or a sulfur atom,

L is a hydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group,

G is ##STR4## A is a CH group, or a nitrogen atom, and each of B and D which are independent of each other, is a C₁₋₄ alkyl group, a C₁₋₄ alkoxy group, a mono-, di- or poly-halogeno C₁₋₄ alkyl group, a mono-, di- or poly-halogeno C₁₋₄ alkoxy group, a halogen atom, a C₁₋₄ alkylamino group, or a di(C₁₋₄ alkyl)amino group, (hereinafter referred to as the compound of the present invention) exhibits remarkably strong herbicidal activities against many weeds in soil treatment, in soil admixing treatment or in foliage treatment and at the same time has a high level of safety for important crop plants such as wheat, corn, cotton, soybean, sugar beet and rice, etc. The present invention has been accomplished on the basis of this discovery.

Examples for the substituents R^(a1), R^(a2), R^(a3), R^(a4), R^(a5), R^(a6), R^(b1), R^(b2), R^(b3), R^(b4), R^(b5), R^(c1), R^(c2), R^(c3), R^(c4), R^(c5), R^(c6), R^(c7), R^(c8), R^(c9), R^(c10), R^(c11), R^(c12), R^(c13), R^(c14), R^(d1), R^(d2), R^(d3), R^(d4), R^(d5), R^(d6), R^(e1), R^(e2), R^(e3), R^(e4), R^(e5), R^(e6), R^(e7), R^(e8), R^(e9), R^(e10), R^(f1), R^(f2), R^(f3), R^(f4), R^(f5), R^(f6), R^(f7), R^(f8), R^(f9), R^(f10), R^(f11), R^(f12), R^(f13), R^(f14), R^(f15), R^(g1), R^(g2), R^(g3) L, B and D the compound of the present invention are as follows. However, symbols have the following meanings.

Me: methyl group, Et: ethyl group, Pr-n: n-propyl group, Pr-iso: isopropyl group, Bu-n: n-butyl group, Bu-iso: isobutyl group, Bu-sec: sec-butyl group, Bu-tert: tert-butyl group, Pen-n: n-pentyl group, Hex-n: n-hexyl group, Hep-n: n-heptyl group, Pr-cyc: cyclopropyl group, Bu-cyc: cyclobutyl group, Pen-cyc: cyclopentyl group, Hex-cyc: cyclohexyl group, and Ph: phenyl group.

Specific examples for the substituents R^(a1), R^(b1), R^(d1), R^(e1) and R^(f1) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc, CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMeCH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂ Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR5## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe, CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂ OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂ CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂ OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂ OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₂ CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂ CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂ CH₂ Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂ CH₂ OCH, CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂ CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂ OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂ CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF₂, CH₂ CH₂ OCH₂ CH═CF₂, CH₂ OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂ C.tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂ C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂ C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂ CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ Me, CH₂ CHMeSO₂ Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂ CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂ CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂ CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C(CF₃)Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂ CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂ CN, CHMeCN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN)CH═CH₂, CH₂ C(CN)═CH₂, CH₂ C(CN)═CHMe, CH₂ CH(CN)C.tbd.CH, CH₂ CH(CN)C═C-Me, CH(CN)C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂ CH₂ NO₂, CH₂ CH.tbd.CHNO₂, CH₂ CH(NO₂)CH.tbd.CH₂, CH₂ C(NO₂)═CH₂, CH₂ C(NO₂)═CHMe, CH₂ CH(NO₂)C.tbd.CH, CH₂ CH(NO₂)C.tbd.CMe, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂ Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CH₂ CO₂ Me, CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me, CH₂ CMe=CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me, CH₂ CH═CHCH₂ CO₂ Me, CH₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂ C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂ COCF₃, CH₂ COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂ COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂ COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂ COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂ CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ OCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂ COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂ COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂ CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂ COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂ Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂ CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt, CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt, CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂ NHPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂ NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂ NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂ NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂ N(OMe)Me, CH₂ SO₂ N(OMe)Et, CH₂ SO₂ N(OEt)Me, CH₂ CH₂ SO₂ N(OMe)Me, CH₂ CH₂ SO₂ N(OMe)Et, CH₂ CH₂ SO₂ N(OEt)Me, CH₂ SO₂ N(OEt)Et, CH₂ CH₂ SO₂ N(OEt)Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂ CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMeEt, CH₂ CONEt₂, CH₂ CH₂ CONMe₂, CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂ CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂ CON(OMe)Me, CH₂ CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CH₂ CON(OMe)Me, CH₂ CH₂ CON(OMe)Et, CH₂ CH₂ CON(OEt)Me, CH₂ CON(OEt)Et, CH₂ CH₂ CON(OEt)Et, CH₂ NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n, CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe, CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n, CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂ NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂ NEt₂, CH₂ N(OMe)Me, CH₂ N(OMe)Et, CH₂ N(OEt)Me, CH₂ N(OEt)Et, CH₂ CH₂ N(OMe)Me, CH₂ CH₂ N(OMe)Et, CH₂ CH₂ N(OEt)Me, CH₂ CH₂ N(OEt)Et, CH₂ NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂ CH₂ NMeCOEt, CH₂ N(OMe)COMe, CH₂ N(OEt)COMe, CH₂ N(OMe)COEt, CH₂ CH₂ N(OMe)COMe, CH₂ CH₂ N(OEt)COMe, CH₂ CH₂ N(OMe)COEt, CH₂ NMeSO₂ Me, CH₂ NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂ CH₂ NMeSO₂ Et, CH₂ N(OMe)SO₂ Me, CH₂ N(OEt)SO₂ Me, CH₂ N(OMe)SO₂ Et, CH₂ CH₂ N(OMe)SO₂ Me, CH₂ CH₂ N(OEt)SO₂ Me, CH₂ CH₂ N(OMe)SO₂ Et, CH₂ Ph, CH₂ CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh, CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe=CMePh, CHMeCMe=CMePh, CH₂ C.tbd.CPh, CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh, CH₂ CMe₂ OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂ SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂ CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂ SCH₂ Ph, CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂ CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph, CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph, CHMeCOCH₂ Ph, CH₂ C(Cl)═CH₂, Ph, CH₂ SOPh, CH₂ SO₂ Ph, CH₂ Ph-4-OMe, CH₂ Ph-4-Cl, CH₂ C(Br)═CH₂, CH₂ C(Cl)═CHCl, CH₂ CH═C(I)Me, CH₂ CH═CHI, CH₂ C(F)═CHCl, CH₂ CH═CBr₂, CH₂ CH═CHF, CH₂ C(Cl)═CHMe, CH₂ C(F)═CHBr, CH₂ C(Br)═CHCl, CH₂ C(Br)═CCl₂, CH₂ CH=CHCH₂ F, CH₂ C(I)═CH₂, CH₂ C(Br)═C(Cl)Me, CH₂ C(I)═CHMe, CH₂ C(Cl)═CCl₂, CH₂ CH═CHCCl₃, CH₂ C(Br)═CHMe, CH₂ C(Cl)═CHF, CH₂ C(Br)═CHF, CH₂ CH═C(Cl)Br, CH₂ C(F)═C(Cl)CF₃, CH₂ C(Cl)═C(Cl)Me, CH₂ C(Br)═CHBr, CH₂ CH═C(F)CF₂ Cl, CH₂ C(Br)═C(Br)Me, CH₂ CH═C(F)CF₃, CH₂ CH═CCl₂, CH₂ C(F)═CH₂, CH₂ CH═CHCCl₃, CH₂ CH═C(F)Cl, CH₂ C(Cl)═C(F)Cl, CH₂ C(F)═CCl₂, CH₂ C(Cl)═CF₂, CH₂ C(CF₃)═CH₂, CMe₂ CH═CH₂, CMe₂ C.tbd.CH, CH₂ CH₂ I, CH₂ C.tbd.C--CN, CH₂ NHBu-n, CH₂ NHSO₂ Me, CH₂ NHSO₂ Et, CH₂ CH₂ NHSO₂ Me, CH₂ CH₂ NHSO₂ Et, CH₂ NHCOMe, CH₂ NHCOEt, CH₂ CH₂ NHCOMe, CH₂ CH₂ NHCOEt

Specific examples for the substituents R^(a2) and R^(a3) of the compound of the present invention

H, Me, Et, Pr-n, Pr-i so, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, B r, I, NO₂, CN, Ph

Specific examples for the substituents R^(a4) and R^(a5) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe=CH₂, CH═CMe₂, CMe=CHMe, CMe=CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(a6) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CMe₂ CH═CH₂, CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(b2) of the compound of the present invention

H, Me, Et, Pr-n, Pr-i so, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH, F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituent R^(b3) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH², CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC═CMe

Specific examples for the substituent R^(b4) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Pen-n, Hex-n

Specific examples for the substituent R^(b5) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Pen-n, Hex-n

Specific examples for the substituent R^(c1) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc, CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMeCH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂ Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR6## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe, CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂ OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂, CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂ OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂ OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C═CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₂ CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂ CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂ CH₂ Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂ CH₂ OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂ CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂ OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂ CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF₂, CH₂ CH₂ OCH₂ CH═CF₂, CH₂ OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂ C.tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂ C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂ C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂ CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ Me, CH₂ CHMeSO₂ Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂ CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂ CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₃, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂ CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C(CF₃)Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂ CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂ CN, CHMeCN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN)CH═CH₂, CH₂ C(CN)═CH₂, CH₂ C(CN)═CHMe, CH₂ CH(CN)C.tbd.CH, CH₂ CH(CN)C.tbd.C-Me, CH(CN)C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂ CH₂ NO₂, CH₂ CH═CHNO₂, CH₂ CH(NO₂)CH═CH₂, CH₂ C(NO₂)═CH₂, CH₂ C(NO₂)═CHMe, CH₂ CH(NO₂)C.tbd.CH, CH₂ CH(NO₂)C.tbd.CMe, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂ Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CH₂ CO₂ Me, CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me, CH═CMe=CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me, CH₂ CH═CHCH₂ CO₂ Me, CH₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂ C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂ COCF₃, CH₂ COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂ COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂ COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂ COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂ CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂ COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂ COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂ CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂ COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂ Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂ CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt, CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt, CHMeC.tbd.CCOMe, CHMeCζCCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂ NHPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂ NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂ NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂ NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂ N(OMe)Me, CH₂ SO₂ N(OMe)Et, CH₂ SO₂ N(OEt)Me, CH₂ CH₂ SO₂ N(OMe)Me, CH₂ CH₂ SO₂ N(OMe)Et, CH₂ CH₂ SO₂ N(OEt)Me, CH₂ SO₂ N(OEt)Et, CH₂ CH₂ SO₂ N(OEt)Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂ CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMeEt, CH₂ CONEt₂, CH₂ CH₂ CONMe₂, CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂ CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂ CON(OMe)Me, CH₂ CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CH₂ CON(OMe)Me, CH₂ CH₂ CON(OMe)Et, CH₂ CH₂ CON(Oet)Me, CH₂ CON(OEt)Et, CH₂ CH₂ CON(OEt)Et, CH₂ NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n, CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe, CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n, CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂ NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂ NEt₂, CH₂ N(OMe)Me, CH₂ N(OMe)Et, CH₂ N(OEt)Me, CH₂ N(OEt)Et, CH₂ CH₂ N(OMe)Me, CH₂ CH₂ N(OMe)Et, CH₂ CH₂ N(OEt)Me, CH₂ CH₂ N(OEt)Et, CH₂ NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂ CH₂ NMeCOEt, CH₂ N(OMe)COMe, CH₂ N(OEt)COMe, CH₂ N(OMe)COEt, CH₂ CH₂ N(OMe)COMe, CH₂ CH₂ N(OEt)COMe, CH₂ CH₂ N(OMe)COEt, CH₂ NMeSO₂ Me, CH₂ NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂ CH₂ NMeSO₂ Et, CH₂ N(OMe)SO₂ Me, CH₂ N(OEt)SO₂ Me, CH₂ N(OMe)SO₂ Et, CH₂ CH₂ N(OMe)SO₂ Me, CH₂ CH₂ N(OEt)SO₂ Me, CH₂ CH₂ N(OMe)SO₂ Et, CH₂ Ph, CH₂ CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh, CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe=CMePh, CHMeCMe=CMePh, CH₂ C.tbd.CPh, CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh, CH₂ CMe₂ OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂ SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂ CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ COCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂ SCH₂ Ph, CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂ CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph, CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph, CHMeCOCH₂ Ph, CH₂ C(Cl)═CH₂, Ph, CH₂ SOPh, CH₂ SO₂ Ph, CH₂ C(Cl)═CHCl, CH₂ CH═C(I)Me, CH₂ CH═CHI, CH₂ C(F)═CHCl, CH₂ CH═CBr₂, CH₂ CH═CHF, CH₂ C(Cl)═CHMe, CH₂ C(F)═CHBr, CH₂ C(Br)═CHCl, CH₂ C(Br)═CCl₂, CH₂ CH═CHCH₂ F, CH₂ C(Br)═CH₂, CH₂ C(I)═CH₂, CH₂ C(Br)═C(Cl)Me, CH═C(I)═CHMe, CH₂ C(Cl)═CCl₂, CH₂ CH═CHCCl₃, CH₂ C(Br)═CHMe, CH₂ C(Cl)═CHF, CH₂ C(Br)═CHF, CH₂ CH═C(Cl)Br, CH₂ C(F)═C(Cl)CF₃, CH₂ C(Cl)═C(Cl)Me, CH₂ C(Br)═CHBr, CH₂ CH═C(F)CF₂ Cl, CH₂ C(Br)═C(Br)Me, CH₂ CH═C(F)CF₃, CH₂ CH═CCl₂, CH₂ C(F)═CH₂, CH₂ CH═CHCCl₃, CH₂ CH═C(F)Cl, CH₂ C(Cl)═C(F)Cl, CH₂ C(F)═CCl₂, CH₂ C(Cl)═CF₂, CH₂ C(CF₃)═CH₂, CMe₂ CH═CH₂, CMe₂ C.tbd.CH, CH₂ CH₂ I, CH₂ C.tbd.C--CN, CH₂ NHBu-n, CH₂ NHSO₂ Me, CH₂ NHSO₂ Et, CH₂ CH₂ NHSO₂ Me, CH₂ CH₂ NHSO₂ Et, CH₂ NHCOMe, CH₂ NHCOEt, CH₂ CH₂ NHCOMe, CH₂ CH₂ NHCOEt

Specific examples for the substituents R^(c2), R^(c3), R^(c4), R^(c5), R^(c6), R^(c11), and R^(c12) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH═CH₂, CH═CHMe, CMe=CH₂, CH═CMe₂, CH═CHEt, CMe=CHMe, CMe=CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CMe₂ CH═CH₂, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CHMeC.tbd.CH, CMe₂ C.tbd.CH, Ph

Specific examples for the substituents R^(c7), R^(c8), R^(c9), R^(c10), R^(c13), and R^(c14) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(d2), R^(d3) and R^(d4) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe=CH₂, CH═CMe₂, CMe=CHMe, CMe=CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples of the substituent R^(d5) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CMe₂ CH═CH₂, CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C═CH, CMe₂ C.tbd.CMe, Ph

Specifics examples for the substituents R^(d6) and R^(f2) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CMe₂ CH═CH₂, CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ SBu-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ SO₂ Bu-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OBu-n, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂ Et, CHMeCO₂ Pr-n, CMe₂ CO₂ Me, CMe₂ CO₂ Et, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ COBu-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CH₂ COPr-n, CH₂ CN, CH₂ CH₂ CN, CH₂ CH₂ CH₂ CN, Ph, CH₂ Ph, CH₂ CH₂ Ph, CHMePh

Specific examples for the substituents R^(e2), R^(e3), R^(e6) and R^(e7) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(e4), R^(e5), R^(e8), R^(e9) and R^(e10) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe=CH₂, CH═CMe₂, CMe=CHMe, CMe=CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituents R^(f3), R^(f4), R^(f7), R^(f8), R^(f11) and R^(f12) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(f5), R^(f6), R^(f9), R^(f10), R^(f13), R^(f14) and R^(f15) of the compound of the present invention

H, Me, Et, pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex, n-Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe=CH₂, CH═CMe₂, CMe=CHMe, CMe=CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(g1) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc, CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMeCH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂ Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR7## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe, CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂ OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂ CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂ OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂ OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₃ CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂ CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂ CH₂ Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂ CH₂ OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂ CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂ OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂ CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF₂, CH₂ CH₂ OCH₂ CH═CF₂, CH₂ OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂ C.tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂ C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂ C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂ CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ Me, CH₂ CHMeSO₂ Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂ CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂ CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂ CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C(CF₃)Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂ CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂ CN, CHMeCN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN)CH═CH₂, CH₂ C(CN)═CH₂, CH₂ C(CN)═CHMe, CH₂ CH(CN)C.tbd.CH, CH₂ CH(CN)C.tbd.C-Me, CH(CN)C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂ CH₂ NO₂, CH₂ CH═CHNO₂, CH₂ CH(NO₂)CH═CH₂, CH₂ C(NO₂)═CH₂, CH₂ C(NO₂)═CHMe, CH₂ CH(NO₂)C.tbd.CH, CH₂ CH(NO₂)C.tbd.CMe, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂ Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CO₂ Me, CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me, CH₂ CMe=CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me, CH₂ CH═CHCH═CO₂ Me, CH₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂ C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂ COCF₃, CH₂ COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂ COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂ COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂ COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂ CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂ COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂ COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂ CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂ COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂ Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂ CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt, CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt, CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂ NHPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂ NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂ NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂ NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂ N(OMe)Me, CH₂ SO₂ N(OMe)Et, CH₂ SO₂ N(OEt)Me, CH₂ CH₂ SO₂ N(OMe)Me, CH₂ CH₂ SO₂ N(OMe)Et, CH₂ CH₂ SO₂ N(OEt)Me, CH₂ SO₂ N(OEt)Et, CH₂ CH₂ SO₂ N(OEt)Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂ CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMeEt, CH₂ CONEt₂, CH₂ CH₂ CONMe₂, CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂ CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂ CON(OMe)Me, CH₂ CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CH₂ CON(OMe)Me, CH₂ CH₂ CON(OMe)Et, CH₂ CH₂ CON(OEt)Me, CH₂ CON(OEt)Et, CH₂ CH₂ CON(OEt)Et, CH₂ NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n, CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe, CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n, CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂ NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂ NEt₂, CH₂ N(OMe)Me, CH₂ N(OMe)Et, CH₂ N(OEt)Me, CH₂ N(OEt)Et, CH₂ CH₂ N(OMe)Me, CH₂ CH₂ N(OMe)Et, CH₂ CH₂ N(OEt)Me, CH₂ CH₂ N(OEt)Et, CH₂ NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂ CH₂ NMeCOEt, CH₂ N(OMe)COMe, CH₂ N(OEt)COMe, CH₂ N(OMe)COEt, CH₂ CH₂ N(OMe)COMe, CH₂ CH₂ N(OEt)COMe, CH₂ CH₂ N(OMe)COEt, CH₂ NMeSO₂ Me, CH₂ NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂ CH₂ NMeSO₂ Et, CH₂ N(OMe)SO₂ Me, CH₂ N(OEt)SO₂ Me, CH₂ N(OMe)SO₂ Et, CH₂ CH₂ N(OMe)SO₂ Me, CH₂ CH₂ N(OEt)SO₂ Me, CH₂ CH₂ N(OMe)SO₂ Et, CH₂ Ph, CH₂ CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh, CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe=CMePh, CHMeCMe=CMePh, CH₂ C.tbd.CPh, CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh, CH₂ CMe₂, OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂ SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂ CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂ SCH₂ Ph, CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂ CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph, CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph, CHMeCCOCH₂ Ph

Specific examples for the substituents R^(g2) and R^(g3) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe=CH₂, CH₂ CMe=CHMe, CHMeCH═CHMe, CH₂ CMe=CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe=CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, SO₂ NHMe, SO₂ NHEt, SO₂ NHPr-n, SO₂ NHPr-iso, SO₂ NMe₂, SO₂ NEt₂, SO₂ N(Pr-n)₂, SO₂ NMeEt, SO₂ NMePr-n, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, CONHMe, CONHEt, CONHPr-n, CONHPr-iso, CONMe₂, CONEt₂, CON(Pr-n)₂, CONMeEt, CONMePr-n, Ph, PhCH₂

Specific examples of --NR^(g2) R^(g3) wherein the substituents R^(g2) and R^(g3) of the compound of the present invention form a saturated 3- to 7-membered heterocyclic ring together with the nitrogen atom to which they are bonded ##STR8## Specific examples for the substituent L of the compound of the present invention

H, Me, Et, Pr-n, CH₂ CH═CH₂, CH₂ C.tbd.CH

Specific examples for the substituents B and D of the compound of the present invention

Me, Et, Pr-n, OMe, OEt, CH₂ F, CHF₂, CF₃, OCHF₂, OCF₃, F, Cl, Br, NHMe, NHEt, NHPr-n, OCH₂ CF₃, NMe₂, OCBrF₂, CH₂ Cl, CH₂ F

Now, examples of the compound covered by the present invention will be presented in the following Tables 1A, 1B, 1C, 2A, 2B, 2C, 3, 4A, 4B, 4C, 5, 6, 7, 8, 9, 10, 11 and 12. However, the compound of the present invention is not limited to such examples. The symbols in these Tables have the following meanings.

Me: methyl group, Et: ethyl group, Pr-n: n-propyl group, Pr-iso: isopropyl group, Bu-n: n-butyl group, Bu-iso: isobutyl group, Bu-sec: sec-butyl group, Bu-tert: tert-butyl group, Pen-n: n-pentyl group, Hex-n: n-hexyl group, Hep-n: n-heptyl group, Pr-cyc: cyclopropyl group, Bu-cyc: cyclobutyl group, Pen-cyc: cyclopentyl group, Hex-cyc: cyclohexyl group, and Ph: phenyl group, ##STR9##

Gn is the same as above G and represents the following Ga, Gb and Gc.

Ga=G1 to G90 (i.e. represents any one of G1 to G90)

Gb=G1 to G13 (i.e. represents any one of G1 to G13)

Gc=G1 to G6 (i.e. represents any one of G1 to G6) ##STR10##

                  TABLE 1A                                                         ______________________________________                                          ##STR11##                                                                      ##STR12##                                                                      ##STR13##                                                                      ##STR14##                                                                      ##STR15##                                                                      ##STR16##                                                                      ##STR17##                                                                      ##STR18##                                                                      ##STR19##                                                                      ##STR20##                                                                      ##STR21##                                                                      ##STR22##                                                                      ##STR23##                                                                      ##STR24##                                                                      ##STR25##                                                                      ##STR26##                                                                      ##STR27##                                                                      ##STR28##                                                                      ##STR29##                                                                      ##STR30##                                                                      ##STR31##                                                                      ##STR32##                                                                      ##STR33##                                                                      ##STR34##                                                                      ##STR35##                                                                      ##STR36##                                                                      ##STR37##                                                                      ##STR38##                                                                      ##STR39##                                                                      ##STR40##                                                                      ##STR41##                                                                      ##STR42##                                                                      ##STR43##                                                                      ##STR44##                                                                      ##STR45##                                                                      ##STR46##                                                                      ##STR47##                                                                      ##STR48##                                                                      ##STR49##                                                                      ##STR50##                                                                      ##STR51##                                                                      ##STR52##                                                                      ##STR53##                                                                      ##STR54##                                                                      ##STR55##                                                                      ##STR56##                                                                      ##STR57##                                                                      ##STR58##                                                                      ##STR59##                                                                      ##STR60##                                                                      ##STR61##                                                                      ##STR62##                                                                     ______________________________________                                         R.sup.m                   Gn                                                   ______________________________________                                         Me                        Ga                                                   Et                        Ga                                                   Pr-n                      Ga                                                   Pr-iso                    Ga                                                   Bu-n                      Ga                                                   Bu-iso                    Ga                                                   Bu-sec                    Gb                                                   Bu-tert                   Gb                                                   Pen-n                     Ga                                                   Hex-n                     Gb                                                   Hep-n                     Gb                                                   Prcyc                     Ga                                                   Hexcyc                    Ga                                                   CH.sub.2 Prcyc            Ga                                                   CH.sub.2 CH.sub.2 Prcyc   Ga                                                   CH.sub.2 Bu-cyc           Gb                                                   CH.sub.2 Pen-cyc          Gc                                                   Hexen-cyc                 Gb                                                   CH.sub.2 Penten-cyc       Gb                                                   CH.sub.2 CHCH.sub.2       Ga                                                   CH.sub.2 CHCHMe           Ga                                                   CH.sub.2 CHCHEt           Ga                                                   CH.sub.2 CHCMe.sub.2      Gb                                                   CH.sub.2 CMeCH.sub.2      Ga                                                   CH.sub.2 CHMeCHCHMe       Gc                                                   CH.sub.2 CH.sub.2 CHCH.sub.2                                                                             Ga                                                   CH.sub.2 CH.sub.2 CHCHMe  Gb                                                   CH.sub.2 CCH              Ga                                                   CH.sub.2 CCMe             Ga                                                   CH.sub.2 CCEt             Ga                                                   CH.sub.2 CH.sub.2 CH      Ga                                                   CH.sub.2 CH.sub.2 CCMe    Gb                                                   CHMeCCH                   Gb                                                   CHMeCCMe                  Gc                                                   CH.sub.2 OMe              Ga                                                   CH.sub.2 OEt              Ga                                                   CH.sub.2 OPr-n            Gb                                                   CH.sub.2 CH.sub.2 OMe     Ga                                                   CH.sub.2 CH.sub.2 OEt     Ga                                                   CH.sub.2 CH.sub.2 OPr-n   Gb                                                   CH.sub.2 CHMeOMe          Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                           Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                           Ga                                                   CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                            Ga                                                   CH.sub.2 OCH.sub.2 CHCHMe Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                       Ga                                                   CH.sub.2 OCH.sub.2 CCH    Ga                                                   CH.sub.2 OCH.sub.2 CCMe   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                          Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                         Ga                                                   CH.sub.2 OCHF.sub.2       Ga                                                   CH.sub.2 OCF.sub.3        Ga                                                   CH.sub.2 CH.sub.2 OCHF.sub.2                                                                             Ga                                                   CH.sub.2 CH.sub.2 OCF.sub.3                                                                              Ga                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                              Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                     Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                            Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                           Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                  Ga                                                   CH.sub.2 OCH.sub.2 CHCHCl Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                       Gb                                                   CH.sub.2 OCH.sub.2 CHCHBr Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                       Gb                                                   CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                            Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                   Gb                                                   CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                          Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                 Gb                                                   CH.sub.2 OCH.sub.2 CCI    Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                          Gb                                                   CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                            Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                   Gb                                                   CH.sub.2 SMe              Ga                                                   CH.sub.2 SEt              Ga                                                   CH.sub.2 SPr-n            Gb                                                   CH.sub.2 CH.sub.2 SMe     Ga                                                   CH.sub.2 CH.sub.2 SEt     Ga                                                   CH.sub.2 CH.sub.2 SPr-n   Gb                                                   CH.sub.2 SOMe             Gb                                                   CH.sub.2 SOEt             Gb                                                   CH.sub.2 CH.sub.2 SOMe    Gb                                                   CH.sub.2 CH.sub.2 SOEt    Gb                                                   CH.sub.2 SO.sub.2 Me      Ga                                                   CH.sub.2 SO.sub.2 Et      Ga                                                   CH.sub.2 SO.sub.2 Pr-n    Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                          Gb                                                   CH.sub.2 CH.sub.2 F       Ga                                                   CH.sub.2 CHF.sub.2        Ga                                                   CH.sub.2 CF.sub.3         Ga                                                   CH.sub.2 CH.sub.2 Cl      Ga                                                   CH.sub.2 CH.sub.2 Br      Ga                                                   CH.sub.2 CH.sub.2 CF.sub.3                                                                               Ga                                                   CH.sub.2 CF.sub.2 CF.sub.3                                                                               Ga                                                   CH.sub.2 CHCHCl           Ga                                                   CH.sub.2 CHCHBr           Ga                                                   CH.sub.2 CHCF.sub.2       Ga                                                   CH.sub.2 CHCHCF.sub.3     Ga                                                   CH.sub.2 CCI              Gb                                                   CH.sub.2 CCCF.sub.3       Gb                                                   CH.sub.2 CN               Ga                                                   CH.sub.2 CH.sub.2 CN      Ga                                                   CHMeCN                    Ga                                                   CH.sub.2 CHCHCN           Ga                                                   CH(CN)CCH                 Gb                                                   CH.sub.2 NO.sub.2         Ga                                                   CH.sub.2 CH.sub.2 NO.sub.2                                                                               Ga                                                   CH.sub.2 CHCHNO.sub.2     Gb                                                   CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                          Gc                                                   CH.sub.2 CH(NO.sub.2)CCH  Gc                                                   CH.sub.2 CO.sub.2 Me      Gb                                                   CH.sub.2 CO.sub.2 Et      Gb                                                   CH.sub.2 CO.sub.2 Pr-n    Gb                                                   CHMeCO.sub.2 Me           Gb                                                   CHMeCO.sub.2 Et           Gb                                                   CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                            Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                            Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                   Gb                                                   CH.sub.2 CHCHCO.sub.2 Me  Ga                                                   CH.sub.2 CHCHCO.sub.2 Et  Ga                                                   CHMeCHCHCO.sub.2 Me       Ga                                                   CHMeCHCHCO.sub.2 Et       Ga                                                   CH.sub.2 CCCO.sub.2 Me    Ga                                                   CH.sub.2 CCCO.sub.2 Et    Ga                                                   CH.sub.2 COMe             Ga                                                   CH.sub.2 COEt             Ga                                                   CH.sub.2 COPr-n           Gb                                                   CH.sub.2 CH.sub.2 COMe    Ga                                                   CH.sub.2 CH.sub.2 COEt    Ga                                                   CH.sub.2 COCF.sub.3       Ga                                                   CH.sub.2 CH.sub.2 COCF.sub.3                                                                             Ga                                                   CH.sub.2 COCH.sub.2 CF.sub.3                                                                             Gb                                                   CH.sub.2 COCH.sub.2 F     Gb                                                   CH.sub.2 COCHCH.sub.2     Ga                                                   CH.sub.2 COCHCHMe         Ga                                                   CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                           Gb                                                   CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                           Gb                                                   CH.sub.2 CH.sub.2 COCHCHMe                                                                               Gb                                                   CH.sub.2 COCCH            Ga                                                   CH.sub.2 COCCMe           Ga                                                   CH.sub.2 COCH.sub.2 OMe   Ga                                                   CH.sub.2 COCH.sub.2 OEt   Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                         Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                         Ga                                                   CH.sub.2 COCH.sub.2 SMe   Ga                                                   CH.sub.2 COCH.sub.2 SEt   Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                         Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                         Ga                                                   CH.sub.2 COCH.sub.2 SOMe  Gb                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                        Gb                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                          Ga                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                          Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                 Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                                 Ga                                                   CH.sub.2 CHCHCOMe         Ga                                                   CH.sub.2 CHCHCOEt         Ga                                                   CHMeCHCHCOMe              Ga                                                   CHMeCHCHCOEt              Ga                                                   CH.sub.2 CCCOMe           Ga                                                   CH.sub.2 CCCOEt           Ga                                                   CH.sub.2 SO.sub.2 NHMe    Ga                                                   CH.sub.2 SO.sub.2 NHEt    Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                          Ga                                                   CH.sub.2 SO.sub.2 NHOMe   Ga                                                   CH.sub.2 SO.sub.2 NHOEt   Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                         Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                         Ga                                                   CH.sub.2 SO.sub.2 NMe.sub.2                                                                              Ga                                                   CH.sub.2 SO.sub.2 NMeEt   Ga                                                   CH.sub.2 SO.sub.2 NEt.sub.2                                                                              Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                     Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                         Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                     Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Me                                                                               Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Et                                                                               Ga                                                   CH.sub.2 SO.sub.2 N(OEt)Me                                                                               Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                      Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                      Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                      Ga                                                   CH.sub.2 CONHMe           Ga                                                   CH.sub.2 CONHEt           Ga                                                   CH.sub.2 CONHPr-n         Gb                                                   CH.sub.2 CH.sub.2 CONHMe  Ga                                                   CH.sub.2 CH.sub.2 CONHEt  Ga                                                   CH.sub.2 CH.sub.2 CONHPr-n                                                                               Gb                                                   CH.sub.2 CONMe.sub.2      Ga                                                   CH.sub.2 CONMeEt          Ga                                                   CH.sub.2 CONEt.sub.2      Ga                                                   CH.sub.2 CONHOMe          Ga                                                   CH.sub.2 CONHOEt          Ga                                                   CH.sub.2 CONHOPr-n        Gb                                                   CH.sub.2 CON(OMe)Me       Ga                                                   CH.sub.2 CON(OMe)Et       Ga                                                   CH.sub.2 CON(OEt)Me       Ga                                                   CH.sub.2 CON(OEt)Et       Ga                                                   CH.sub.2 NHMe             Ga                                                   CH.sub.2 NHEt             Ga                                                   CH.sub.2 NHPr-n           Gb                                                   CH.sub.2 CH.sub.2 NHMe    Ga                                                   CH.sub.2 CH.sub.2 NHEt    Ga                                                   CH.sub.2 CH.sub.2 NHPr-n  Gb                                                   CH.sub.2 NHOMe            Ga                                                   CH.sub.2 NHOEt            Ga                                                   CH.sub.2 CH.sub.2 NHOMe   Ga                                                   CH.sub.2 CH.sub.2 NHOEt   Ga                                                   CH.sub.2 NMe.sub.2        Ga                                                   CH.sub.2 NMeEt            Ga                                                   CH.sub.2 CH.sub.2 NMe.sub.2                                                                              Ga                                                   CH.sub.2 CH.sub.2 NMeEt   Ga                                                   CH.sub.2 N(OMe)Me         Ga                                                   CH.sub.2 N(OMe)Et         Ga                                                   CH.sub.2 N(OEt)Me         Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Me                                                                               Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Et                                                                               Ga                                                   CH.sub.2 CH.sub.2 N(OEt)Me                                                                               Ga                                                   CH.sub.2 NMeCOMe          Ga                                                   CH.sub.2 NEtCOMe          Ga                                                   CH.sub.2 NMeCOEt          Ga                                                   CH.sub.2 CH.sub.2 NMeCOMe Ga                                                   CH.sub.2 CH.sub.2 NEtCOMe Ga                                                   CH.sub.2 CH.sub.2 NMeCOEt Ga                                                   CH.sub.2 N(OMe)COMe       Ga                                                   CH.sub.2 N(OEt)COMe       Ga                                                   CH.sub.2 N(OMe)COEt       Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COMe                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OEt)COMe                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COEt                                                                             Ga                                                   CH.sub.2 NMeSO.sub.2 Me   Ga                                                   CH.sub.2 NEtSO.sub.2 Me   Ga                                                   CH.sub.2 NMeSO.sub.2 Et   Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                         Ga                                                   CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                         Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                         Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Me                                                                               Ga                                                   CH.sub.2 N(OEt)SO.sub.2 Me                                                                               Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Et                                                                               Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                      Ga                                                   CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                      Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                      Ga                                                   CH.sub.2 Ph               Gb                                                   CH.sub.2 CH.sub.2 Ph      Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                            Gb                                                   CHMePh                    Gb                                                   CH.sub.2 CHCHPh           Ga                                                   CHMeCHCHPh                Ga                                                   CH.sub.2 CCPh             Ga                                                   CHMeCCPh                  Ga                                                   CH.sub.2 CH.sub.2 OPh     Ga                                                   CH.sub.2 OPh              Ga                                                   CH.sub.2 CH.sub.2 SPh     Ga                                                   CH.sub.2 SPh              Ga                                                   CH.sub.2 CH.sub.2 SOPh    Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                            Ga                                                   CH.sub.2 OCH.sub.2 Ph     Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                           Ga                                                   CH.sub.2 SCH.sub.2 Ph     Ga                                                   CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                           Ga                                                   CH.sub.2 SOCH.sub.2 Ph    Gb                                                   CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                          Gb                                                   CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                   Ga                                                   CH.sub.2 COPh             Ga                                                   CH.sub.2 CH.sub.2 COPh    Ga                                                   CHMeCOPh                  Ga                                                   CH.sub.2 COCH.sub.2 Ph    Gb                                                   CHMeCOCH.sub.2 Ph         Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 F                                                                             Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                            Ga                                                   CH.sub.2 C(Cl)CH.sub.2    Ga                                                   CH.sub.2 C(Br)CH.sub.2    Ga                                                   Ph                        Ga                                                   CH.sub.2 SOPh             Ga                                                   CH.sub.2 SO.sub.2 Ph      Ga                                                   CH.sub.2 Ph-4-OMe         Gb                                                   CH.sub.2 Ph-4-Cl          Gb                                                   CH.sub.2 C(Cl)CHCl        Ga                                                   CH.sub.2 C(F)CHCl         Ga                                                   CH.sub.2 CHCHF            Ga                                                   CH.sub.2 C(Cl)CHMe        Ga                                                   CH.sub.2 CHC(Cl)Me        Ga                                                   CH.sub.2 CFCF.sub.2       Ga                                                   CH.sub.2 CHCHCH.sub.2 F   Ga                                                   CH.sub.2 C(Br)CHMe        Ga                                                   CH.sub.2 C(Cl)CHF         Ga                                                   CH.sub.2 C(Br)CHF         Ga                                                   CH.sub.2 C(Cl)C(Cl)Me     Ga                                                   CH.sub.2 C(Br)CHBr        Ga                                                   CH.sub.2 C(Br)C(Br)Me     Ga                                                   CH.sub.2 CHC(F)CF.sub.3   Ga                                                   CH.sub.2 CHCCl.sub.2      Ga                                                   CH.sub.2 C(F)CH.sub.2     Ga                                                   CH.sub.2 CHC(F)Cl         Ga                                                   CH.sub.2 C(Cl)C(F)Cl      Ga                                                   CH.sub.2 C(F)CCl.sub.2    Ga                                                   CH.sub.2 CClCF.sub.2      Ga                                                   CH.sub.2 C(CF.sub.3)CH.sub.2                                                                             Ga                                                   CH.sub.2 NHSO.sub.2 Me    Gb                                                   CH.sub.2 CH.sub.2 NHSO.sub.2 Me                                                                          Gb                                                   CH.sub.2 NHCOMe           Gb                                                   CH.sub.2 CH.sub.2 NHCOMe  Gb                                                   ______________________________________                                    

                  TABLE 1B                                                         ______________________________________                                          ##STR63##                                                                      ##STR64##                                                                      ##STR65##                                                                      ##STR66##                                                                      ##STR67##                                                                      ##STR68##                                                                      ##STR69##                                                                      ##STR70##                                                                      ##STR71##                                                                      ##STR72##                                                                      ##STR73##                                                                      ##STR74##                                                                      ##STR75##                                                                      ##STR76##                                                                      ##STR77##                                                                      ##STR78##                                                                      ##STR79##                                                                      ##STR80##                                                                      ##STR81##                                                                      ##STR82##                                                                      ##STR83##                                                                      ##STR84##                                                                      ##STR85##                                                                      ##STR86##                                                                      ##STR87##                                                                      ##STR88##                                                                      ##STR89##                                                                      ##STR90##                                                                      ##STR91##                                                                      ##STR92##                                                                      ##STR93##                                                                      ##STR94##                                                                      ##STR95##                                                                      ##STR96##                                                                      ##STR97##                                                                      ##STR98##                                                                      ##STR99##                                                                      ##STR100##                                                                     ##STR101##                                                                     ##STR102##                                                                     ##STR103##                                                                     ##STR104##                                                                     ##STR105##                                                                     ##STR106##                                                                     ##STR107##                                                                     ##STR108##                                                                     ##STR109##                                                                     ##STR110##                                                                     ##STR111##                                                                     ##STR112##                                                                     ##STR113##                                                                     ##STR114##                                                                     ##STR115##                                                                     ##STR116##                                                                     ##STR117##                                                                     ##STR118##                                                                     ##STR119##                                                                     ##STR120##                                                                     ##STR121##                                                                     ##STR122##                                                                     ##STR123##                                                                     ##STR124##                                                                     ##STR125##                                                                     ##STR126##                                                                     ##STR127##                                                                     ##STR128##                                                                     ##STR129##                                                                     ##STR130##                                                                     ##STR131##                                                                     ##STR132##                                                                     ##STR133##                                                                     ##STR134##                                                                     ##STR135##                                                                     ##STR136##                                                                     ##STR137##                                                                     ##STR138##                                                                     ##STR139##                                                                     ##STR140##                                                                     ##STR141##                                                                     ##STR142##                                                                     ##STR143##                                                                     ##STR144##                                                                     ##STR145##                                                                     ##STR146##                                                                     ##STR147##                                                                     ##STR148##                                                                     ##STR149##                                                                     ##STR150##                                                                     ##STR151##                                                                     ##STR152##                                                                     ##STR153##                                                                     ##STR154##                                                                     ##STR155##                                                                     ##STR156##                                                                     ##STR157##                                                                     ##STR158##                                                                     ##STR159##                                                                     ##STR160##                                                                     ##STR161##                                                                     ##STR162##                                                                     ##STR163##                                                                     ##STR164##                                                                     ##STR165##                                                                     ##STR166##                                                                     ##STR167##                                                                     ##STR168##                                                                     ##STR169##                                                                     ##STR170##                                                                     ##STR171##                                                                     ##STR172##                                                                     ##STR173##                                                                     ##STR174##                                                                     ##STR175##                                                                     ##STR176##                                                                     ##STR177##                                                                     ##STR178##                                                                     ##STR179##                                                                     ##STR180##                                                                     ##STR181##                                                                     ##STR182##                                                                     ##STR183##                                                                     ##STR184##                                                                     ##STR185##                                                                     ##STR186##                                                                     ##STR187##                                                                     ##STR188##                                                                     ##STR189##                                                                     ##STR190##                                                                     ##STR191##                                                                     ##STR192##                                                                     ##STR193##                                                                     ##STR194##                                                                     ##STR195##                                                                     ##STR196##                                                                     ##STR197##                                                                     ##STR198##                                                                     ##STR199##                                                                     ##STR200##                                                                     ##STR201##                                                                     ##STR202##                                                                     ##STR203##                                                                     ##STR204##                                                                     ##STR205##                                                                     ##STR206##                                                                     ##STR207##                                                                     ##STR208##                                                                     ##STR209##                                                                    ______________________________________                                         R.sup.m                  Gn                                                    ______________________________________                                         Me                       Ga                                                    Et                       Ga                                                    Pr-n                     Ga                                                    Priso                    Ga                                                    Bu-n                     Ga                                                    Bu-iso                   Gb                                                    Pen-n                    Gb                                                    Hex-n                    Gb                                                    CH.sub.2 Prcyc           Ga                                                    CH.sub.2 CH.sub.2 Prcyc  Ga                                                    CH.sub.2 CHCH.sub.2      Ga                                                    CH.sub.2 CHCHMe          Ga                                                    CH.sub.2 CCH.sub.2       Ga                                                    CH.sub.2 CCMe            Ga                                                    CH.sub.2 OMe             Ga                                                    CH.sub.2 OEt             Ga                                                    CH.sub.2 CH.sub.2 OMe    Ga                                                    CH.sub.2 CH.sub.2 OEt    Ga                                                    CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                           Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                  Ga                                                    CH.sub.2 OCH.sub.2 CCH   Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                         Ga                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                             Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                    Ga                                                    CH.sub.2 SMe             Ga                                                    CH.sub.2 SEt             Ga                                                    CH.sub.2 CH.sub.2 SMe    Ga                                                    CH.sub.2 CH.sub.2 SEt    Ga                                                    CH.sub.2 SO.sub.2 Me     Ga                                                    CH.sub.2 SO.sub.2 Et     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 F      Ga                                                    CH.sub.2 CF.sub.3        Ga                                                    CH.sub.2 CN              Ga                                                    CH.sub.2 CH.sub.2 CN     Ga                                                    CHMeCN                   Ga                                                    CH.sub.2 CHCHCN          Ga                                                    CH.sub.2 NO.sub.2        Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                    CH.sub.2 CO.sub.2 Me     Gb                                                    CH.sub.2 CO.sub.2 Et     Gb                                                    CHMeCO.sub.2 Me          Gb                                                    CHMeCO.sub.2 Et          Gb                                                    CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CHCHCO.sub.2 Me Ga                                                    CH.sub.2 CHCHCO.sub.2 Et Ga                                                    CHMeCHCHCO.sub.2 Me      Ga                                                    CH.sub.2 COMe            Ga                                                    CH.sub.2 COEt            Ga                                                    CH.sub.2 COPr-n          Gb                                                    CH.sub.2 COCF.sub.3      Ga                                                    CH.sub.2 COCHCH.sub.2    Ga                                                    CH.sub.2 COCHCHMe        Ga                                                    CH.sub.2 COCH.sub.2 OMe  Ga                                                    CH.sub.2 COCH.sub.2 OEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SMe  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                         Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                Ga                                                    CH.sub.2 CHCHCOMe        Ga                                                    CHMeCHCHCOMe             Ga                                                    CH.sub.2 SO.sub.2 NHMe   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                         Gb                                                    CH.sub.2 SO.sub.2 NHOMe  Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                        Gb                                                    CH.sub.2 SO.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                    Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                     Ga                                                    CH.sub.2 CONHMe          Gb                                                    CH.sub.2 CH.sub.2 CONHMe Gb                                                    CH.sub.2 CONMe.sub.2     Ga                                                    CH.sub.2 CH.sub.2 CONMe.sub.2                                                                           Ga                                                    CH.sub.2 CONHOMe         Gb                                                    CH.sub.2 CH.sub.2 CONHOMe                                                                               Gb                                                    CH.sub.2 CON(OMe)Me      Ga                                                    CH.sub.2 CH.sub.2 CON(OMe)Me                                                                            Ga                                                    CH.sub.2 NHMe            Gb                                                    CH.sub.2 CH.sub.2 NHMe   Gb                                                    CH.sub.2 NHOMe           Gb                                                    CH.sub.2 CH.sub.2 NHOMe  Gb                                                    CH.sub.2 NMe.sub.2       Ga                                                    CH.sub.2 CH.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 N(OMe)Me        Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 NMeCOMe         Ga                                                    CH.sub.2 CH.sub.2 NMeCOMe                                                                               Ga                                                    CH.sub.2 N(OMe)COMe      Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COMe                                                                            Ga                                                    CH.sub.2 NMeSO.sub.2 Me  Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 Ph              Gb                                                    CH.sub.2 CH.sub.2 Ph     Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                           Gb                                                    CHMePh                   Gb                                                    CH.sub.2 CHCHPh          Gb                                                    CHMeCHCHPh               Gb                                                    CH.sub.2 CH.sub.2 OPh    Gb                                                    CH.sub.2 OPh             Gb                                                    CH.sub.2 CH.sub.2 SPh    Gb                                                    CH.sub.2 SPh             Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                           Gb                                                    CH.sub.2 COPh            Gb                                                    CH.sub.2 CH.sub.2 COPh   Gb                                                    CH.sub.2 COCH.sub.2 Ph   Gb                                                    CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                         Gb                                                    Ph                       Gb                                                    ______________________________________                                    

                  TABLE 1C                                                         ______________________________________                                          ##STR210##                                                                     ##STR211##                                                                     ##STR212##                                                                     ##STR213##                                                                     ##STR214##                                                                     ##STR215##                                                                     ##STR216##                                                                     ##STR217##                                                                     ##STR218##                                                                     ##STR219##                                                                     ##STR220##                                                                     ##STR221##                                                                     ##STR222##                                                                     ##STR223##                                                                     ##STR224##                                                                     ##STR225##                                                                     ##STR226##                                                                     ##STR227##                                                                     ##STR228##                                                                     ##STR229##                                                                     ##STR230##                                                                     ##STR231##                                                                     ##STR232##                                                                     ##STR233##                                                                     ##STR234##                                                                     ##STR235##                                                                     ##STR236##                                                                     ##STR237##                                                                     ##STR238##                                                                     ##STR239##                                                                     ##STR240##                                                                     ##STR241##                                                                     ##STR242##                                                                     ##STR243##                                                                     ##STR244##                                                                     ##STR245##                                                                     ##STR246##                                                                     ##STR247##                                                                     ##STR248##                                                                     ##STR249##                                                                     ##STR250##                                                                     ##STR251##                                                                     ##STR252##                                                                     ##STR253##                                                                     ##STR254##                                                                     ##STR255##                                                                     ##STR256##                                                                     ##STR257##                                                                     ##STR258##                                                                     ##STR259##                                                                     ##STR260##                                                                     ##STR261##                                                                     ##STR262##                                                                     ##STR263##                                                                     ##STR264##                                                                     ##STR265##                                                                     ##STR266##                                                                     ##STR267##                                                                     ##STR268##                                                                     ##STR269##                                                                     ##STR270##                                                                     ##STR271##                                                                     ##STR272##                                                                     ##STR273##                                                                     ##STR274##                                                                     ##STR275##                                                                     ##STR276##                                                                     ##STR277##                                                                     ##STR278##                                                                     ##STR279##                                                                     ##STR280##                                                                     ##STR281##                                                                     ##STR282##                                                                     ##STR283##                                                                     ##STR284##                                                                     ##STR285##                                                                     ##STR286##                                                                     ##STR287##                                                                     ##STR288##                                                                     ##STR289##                                                                     ##STR290##                                                                     ##STR291##                                                                     ##STR292##                                                                     ##STR293##                                                                     ##STR294##                                                                     ##STR295##                                                                     ##STR296##                                                                     ##STR297##                                                                     ##STR298##                                                                     ##STR299##                                                                     ##STR300##                                                                     ##STR301##                                                                     ##STR302##                                                                     ##STR303##                                                                     ##STR304##                                                                     ##STR305##                                                                     ##STR306##                                                                     ##STR307##                                                                     ##STR308##                                                                     ##STR309##                                                                     ##STR310##                                                                     ##STR311##                                                                     ##STR312##                                                                     ##STR313##                                                                     ##STR314##                                                                     ##STR315##                                                                     ##STR316##                                                                     ##STR317##                                                                     ##STR318##                                                                     ##STR319##                                                                     ##STR320##                                                                     ##STR321##                                                                     ##STR322##                                                                     ##STR323##                                                                     ##STR324##                                                                     ##STR325##                                                                     ##STR326##                                                                     ##STR327##                                                                     ##STR328##                                                                     ##STR329##                                                                     ##STR330##                                                                     ##STR331##                                                                     ##STR332##                                                                     ##STR333##                                                                     ##STR334##                                                                     ##STR335##                                                                     ##STR336##                                                                     ##STR337##                                                                     ##STR338##                                                                     ##STR339##                                                                     ##STR340##                                                                     ##STR341##                                                                     ##STR342##                                                                     ##STR343##                                                                     ##STR344##                                                                     ##STR345##                                                                     ##STR346##                                                                     ##STR347##                                                                     ##STR348##                                                                    ______________________________________                                         R.sup.m                  Gn                                                    ______________________________________                                         Me                       Ga                                                    Et                       Ga                                                    Pr-n                     Ga                                                    Priso                    Gb                                                    Bu-n                     Ga                                                    Bu-iso                   Ga                                                    Pen-n                    Gb                                                    CH.sub.2 Prcyc           Ga                                                    CH.sub.2 CH.sub.2 Prcyc  Gb                                                    CH.sub.2 CHCH.sub.2      Ga                                                    CH.sub.2 CHCHMe          Ga                                                    CH.sub.2 CCH             Ga                                                    CH.sub.2 CCMe            Ga                                                    CH.sub.2 CH.sub.2 OMe    Ga                                                    CH.sub.2 OMe             Ga                                                    CH.sub.2 CH.sub.2 SMe    Ga                                                    CH.sub.2 SME             Ga                                                    CH.sub.2 SO.sub.2 Me     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CF.sub.3        Ga                                                    CH.sub.2 CN              Ga                                                    CH.sub.2 CH.sub.2 CN     Ga                                                    CH.sub.2 NO.sub.2        Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                    CH.sub.2 COMe            Ga                                                    CH.sub.2 COEt            Ga                                                    CH.sub.2 COCHCH.sub.2    Ga                                                    CH.sub.2 CHCHCOMe        Ga                                                    CH.sub.2 CONMe.sub.2     Ga                                                    ______________________________________                                    

                  TABLE 2A                                                         ______________________________________                                          ##STR349##                                                                     ##STR350##                                                                     ##STR351##                                                                     ##STR352##                                                                     ##STR353##                                                                    ______________________________________                                         R.sup.cl                  Gn                                                   ______________________________________                                         Me                        Ga                                                   Et                        Ga                                                   Pr-n                      Ga                                                   Pr-iso                    Ga                                                   Bu-n                      Ga                                                   Bu-iso                    Ga                                                   Bu-sec                    Gb                                                   Bu-tert                   Gb                                                   Pen-n                     Ga                                                   Hex-n                     Gb                                                   Hep-n                     Gb                                                   Prcyc                     Ga                                                   Hexcyc                    Ga                                                   CH.sub.2 Prcyc            Ga                                                   CH.sub.2 CH.sub.2 Prcyc   Ga                                                   CH.sub.2 Bu-cyc           Gb                                                   CH.sub.2 Pen-cyc          Gc                                                   Hexen-cyc                 Gb                                                   CH.sub.2 Penten-cyc       Gb                                                   CH.sub.2 CHCH.sub.2       Ga                                                   CH.sub.2 CHCHMe           Ga                                                   CH.sub.2 CHCHEt           Ga                                                   CH.sub.2 CHCMe.sub.2      Ga                                                   CH.sub.2 CMeCH.sub.2      Ga                                                   CH.sub.2 CHMeCHCHMe       Ga                                                   CH.sub.2 CH.sub.2 CHCH.sub.2                                                                             Ga                                                   CH.sub.2 CH.sub.2 CHCHMe  Ga                                                   CH.sub.2 CCH              Ga                                                   CH.sub.2 CCMe             Ga                                                   CH.sub.2 CCEt             Ga                                                   CH.sub.2 CH.sub.2 CH      Ga                                                   CH.sub.2 CH.sub.2 CCMe    Ga                                                   CHMeCCH                   Ga                                                   CHMeCCMe                  Ga                                                   CH.sub.2 OMe              Ga                                                   CH.sub.2 OEt              Ga                                                   CH.sub.2 OPr-n            Gb                                                   CH.sub.2 CH.sub.2 OMe     Ga                                                   CH.sub.2 CH.sub.2 OEt     Ga                                                   CH.sub.2 CH.sub.2 OPr-n   Gb                                                   CH.sub.2 CHMeOMe          Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                           Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                           Ga                                                   CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                            Ga                                                   CH.sub.2 OCH.sub.2 CHCHMe Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                       Ga                                                   CH.sub.2 OCH.sub.2 CCH    Ga                                                   CH.sub.2 OCH.sub.2 CCMe   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                          Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                         Ga                                                   CH.sub.2 OCHF.sub.2       Ga                                                   CH.sub.2 OCF.sub.3        Ga                                                   CH.sub.2 CH.sub.2 OCHF.sub.2                                                                             Ga                                                   CH.sub.2 CH.sub.2 OCF.sub.3                                                                              Ga                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                              Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                     Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                            Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                           Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                  Ga                                                   CH.sub.2 OCH.sub.2 CHCHCl Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                       Gb                                                   CH.sub.2 OCH.sub.2 CHCHBr Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                       Gb                                                   CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                            Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                   Gb                                                   CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                          Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                 Gb                                                   CH.sub.2 OCH.sub.2 CCI    Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                          Gb                                                   CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                            Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                   Gb                                                   CH.sub.2 SMe              Ga                                                   CH.sub.2 SEt              Ga                                                   CH.sub.2 SPr-n            Gb                                                   CH.sub.2 CH.sub.2 SMe     Ga                                                   CH.sub.2 CH.sub.2 SEt     Ga                                                   CH.sub.2 CH.sub.2 SPr-n   Gb                                                   CH.sub.2 SOMe             Gb                                                   CH.sub.2 SOEt             Gb                                                   CH.sub.2 CH.sub.2 SOMe    Gb                                                   CH.sub.2 CH.sub.2 SOEt    Gb                                                   CH.sub.2 SO.sub.2 Me      Ga                                                   CH.sub.2 SO.sub.2 Et      Ga                                                   CH.sub.2 SO.sub.2 Pr-n    Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                          Gb                                                   CH.sub.2 CH.sub.2 F       Ga                                                   CH.sub.2 CHF.sub.2        Ga                                                   CH.sub.2 CF.sub.3         Ga                                                   CH.sub.2 CH.sub.2 Cl      Ga                                                   CH.sub.2 CH.sub.2 Br      Ga                                                   CH.sub.2 CH.sub.2 CF.sub.3                                                                               Ga                                                   CH.sub.2 CF.sub.2 CF.sub.3                                                                               Ga                                                   CH.sub.2 CHCHCl           Ga                                                   CH.sub.2 CHCHBr           Ga                                                   CH.sub.2 CHCF.sub.2       Ga                                                   CH.sub.2 CHCHCF.sub.3     Ga                                                   CH.sub.2 CCI              Gb                                                   CH.sub.2 CCCF.sub.3       Gb                                                   CH.sub.2 CN               Ga                                                   CH.sub.2 CH.sub.2 CN      Ga                                                   CHMeCN                    Ga                                                   CH.sub.2 CHCHCN           Ga                                                   CH(CN)CCH                 Gb                                                   CH.sub.2 NO.sub.2         Ga                                                   CH.sub.2 CH.sub.2 NO.sub.2                                                                               Ga                                                   CH.sub.2 CHCHNO.sub.2     Gb                                                   CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                          Gc                                                   CH.sub.2 CH(NO.sub.2)CCH  Gc                                                   CH.sub.2 CO.sub.2 Me      Ga                                                   CH.sub.2 CO.sub.2 Et      Ga                                                   CH.sub.2 CO.sub.2 Pr-n    Gb                                                   CHMeCO.sub.2 Me           Ga                                                   CHMeCO.sub.2 Et           Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                            Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                            Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                   Gb                                                   CH.sub.2 CHCHCO.sub.2 Me  Ga                                                   CH.sub.2 CHCHCO.sub.2 Et  Ga                                                   CHMeCHCHCO.sub.2 Me       Ga                                                   CHMeCHCHCO.sub.2 Et       Ga                                                   CH.sub.2 CCCO.sub.2 Me    Ga                                                   CH.sub.2 CCCO.sub.2 Et    Ga                                                   CH.sub.2 COMe             Ga                                                   CH.sub.2 COEt             Ga                                                   CH.sub.2 COPr-n           Gb                                                   CH.sub.2 CH.sub.2 COMe    Ga                                                   CH.sub.2 CH.sub.2 COEt    Ga                                                   CH.sub.2 COCF.sub.3       Ga                                                   CH.sub.2 CH.sub.2 COCF.sub.3                                                                             Ga                                                   CH.sub.2 COCH.sub.2 CF.sub.3                                                                             Gb                                                   CH.sub.2 COCH.sub.2 F     Gb                                                   CH.sub.2 COCHCH.sub.2     Ga                                                   CH.sub.2 COCHCHMe         Ga                                                   CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                           Gb                                                   CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                           Gb                                                   CH.sub.2 CH.sub.2 COCHCHMe                                                                               Gb                                                   CH.sub.2 COCCH            Ga                                                   CH.sub.2 COCCMe           Ga                                                   CH.sub.2 COCH.sub.2 OMe   Ga                                                   CH.sub.2 COCH.sub.2 OEt   Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                         Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                         Ga                                                   CH.sub.2 COCH.sub.2 SMe   Ga                                                   CH.sub.2 COCH.sub.2 SEt   Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                         Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                         Ga                                                   CH.sub.2 COCH.sub.2 SOMe  Gb                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                        Gb                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                          Ga                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                          Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                 Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                                 Ga                                                   CH.sub.2 CHCHCOMe         Ga                                                   CH.sub.2 CHCHCOEt         Ga                                                   CHMeCHCHCOMe              Ga                                                   CHMeCHCHCOEt              Ga                                                   CH.sub.2 CCCOMe           Ga                                                   CH.sub.2 CCCOEt           Ga                                                   CH.sub.2 SO.sub.2 NHMe    Ga                                                   CH.sub.2 SO.sub.2 NHEt    Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                          Ga                                                   CH.sub.2 SO.sub.2 NHOMe   Ga                                                   CH.sub.2 SO.sub.2 NHOEt   Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                         Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                         Ga                                                   CH.sub.2 SO.sub.2 NMe.sub.2                                                                              Ga                                                   CH.sub.2 SO.sub.2 NMeEt   Ga                                                   CH.sub.2 SO.sub.2 NEt.sub.2                                                                              Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                     Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                         Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                     Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Me                                                                               Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Et                                                                               Ga                                                   CH.sub.2 SO.sub.2 N(OEt)Me                                                                               Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                      Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                      Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                      Ga                                                   CH.sub.2 CONHMe           Ga                                                   CH.sub.2 CONHEt           Ga                                                   CH.sub.2 CONHPr-n         Gb                                                   CH.sub.2 CH.sub.2 CONHMe  Ga                                                   CH.sub.2 CH.sub.2 CONHEt  Ga                                                   CH.sub.2 CH.sub.2 CONHPr-n                                                                               Gb                                                   CH.sub.2 CONMe.sub.2      Ga                                                   CH.sub.2 CONMeEt          Ga                                                   CH.sub.2 CONEt.sub.2      Ga                                                   CH.sub.2 CONHOMe          Ga                                                   CH.sub.2 CONHOEt          Ga                                                   CH.sub.2 CONHOPr-n        Gb                                                   CH.sub.2 CON(OMe)Me       Ga                                                   CH.sub.2 CON(OMe)Et       Ga                                                   CH.sub.2 CON(OEt)Me       Ga                                                   CH.sub.2 CON(OEt)Et       Ga                                                   CH.sub.2 NHMe             Ga                                                   CH.sub.2 NHEt             Ga                                                   CH.sub.2 NHPr-n           Gb                                                   CH.sub.2 CH.sub.2 NHMe    Ga                                                   CH.sub.2 CH.sub.2 NHEt    Ga                                                   CH.sub.2 CH.sub.2 NHPr-n  Gb                                                   CH.sub.2 NHOMe            Ga                                                   CH.sub.2 NHOEt            Ga                                                   CH.sub.2 CH.sub.2 NHOMe   Ga                                                   CH.sub.2 CH.sub.2 NHOEt   Ga                                                   CH.sub.2 NMe.sub.2        Ga                                                   CH.sub.2 NMeEt            Ga                                                   CH.sub.2 CH.sub.2 NMe.sub.2                                                                              Ga                                                   CH.sub.2 CH.sub.2 NMeEt   Ga                                                   CH.sub.2 N(OMe)Me         Ga                                                   CH.sub.2 N(OMe)Et         Ga                                                   CH.sub.2 N(OEt)Me         Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Me                                                                               Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Et                                                                               Ga                                                   CH.sub.2 CH.sub.2 N(OEt)Me                                                                               Ga                                                   CH.sub.2 NMeCOMe          Ga                                                   CH.sub.2 NEtCOMe          Ga                                                   CH.sub.2 NMeCOEt          Ga                                                   CH.sub.2 CH.sub.2 NMeCOMe Ga                                                   CH.sub.2 CH.sub.2 NEtCOMe Ga                                                   CH.sub.2 CH.sub.2 NMeCOEt Ga                                                   CH.sub.2 N(OMe)COMe       Ga                                                   CH.sub.2 N(OEt)COMe       Ga                                                   CH.sub.2 N(OMe)COEt       Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COMe                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OEt)COMe                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COEt                                                                             Ga                                                   CH.sub.2 NMeSO.sub.2 Me   Ga                                                   CH.sub.2 NEtSO.sub.2 Me   Ga                                                   CH.sub.2 NMeSO.sub.2 Et   Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                         Ga                                                   CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                         Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                         Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Me                                                                               Ga                                                   CH.sub.2 N(OEt)SO.sub.2 Me                                                                               Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Et                                                                               Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                      Ga                                                   CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                      Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                      Ga                                                   CH.sub.2 Ph               Gb                                                   CH.sub.2 CH.sub.2 Ph      Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                            Gb                                                   CHMePh                    Gb                                                   CH.sub.2 CHCHPh           Ga                                                   CHMeCHCHPh                Ga                                                   CH.sub.2 CCPh             Ga                                                   CHMeCCPh                  Ga                                                   CH.sub.2 CH.sub.2 OPh     Ga                                                   CH.sub.2 OPh              Ga                                                   CH.sub.2 CH.sub.2 SPh     Ga                                                   CH.sub.2 SPh              Ga                                                   CH.sub.2 CH.sub.2 SOPh    Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                            Ga                                                   CH.sub.2 OCH.sub.2 Ph     Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                           Ga                                                   CH.sub.2 SCH.sub.2 Ph     Ga                                                   CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                           Ga                                                   CH.sub.2 SOCH.sub.2 Ph    Gb                                                   CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                          Gb                                                   CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                   Ga                                                   CH.sub.2 COPh             Ga                                                   CH.sub.2 CH.sub.2 COPh    Ga                                                   CHMeCOPh                  Ga                                                   CH.sub.2 COCH.sub.2 Ph    Gb                                                   CHMeCOCH.sub.2 Ph         Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 F                                                                             Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                            Ga                                                   CH.sub.2 C(Cl)CH.sub.2    Ga                                                   Ph                        Ga                                                   CH.sub.2 SOPh             Ga                                                   CH.sub.2 SO.sub.2 Ph      Ga                                                   CH.sub.2 C(Cl)CHCl        Ga                                                   CH.sub.2 C(F)CHCl         Ga                                                   CH.sub.2 CHCHF            Ga                                                   CH.sub.2 C(Cl)CHMe        Ga                                                   CH.sub.2 CHC(Cl)Me        Ga                                                   CH.sub.2 CFCF.sub.2       Ga                                                   CH.sub.2 CHCHCH.sub.2 F   Ga                                                   CH.sub.2 C(Br)CHMe        Ga                                                   CH.sub.2 C(Cl)CHF         Ga                                                   CH.sub.2 C(Br)CHF         Ga                                                   CH.sub.2 C(Cl)C(Cl)Me     Ga                                                   CH.sub.2 C(Br)CHBr        Ga                                                   CH.sub.2 C(Br)C(Br)Me     Ga                                                   CH.sub.2 CHC(F)CF.sub.3   Ga                                                   CH.sub.2 CHCCl.sub.2      Ga                                                   CH.sub.2 C(F)CH.sub.2     Ga                                                   CH.sub.2 CHC(F)Cl         Ga                                                   CH.sub.2 C(Cl)C(F)Cl      Ga                                                   CH.sub.2 C(F)CCl.sub.2    Ga                                                   CH.sub.2 CClCF.sub.2      Ga                                                   CH.sub.2 C(CF.sub.3)CH.sub.2                                                                             Ga                                                   CH.sub.2 CHCHI            Ga                                                   CH.sub.2 CHCBr.sub.2      Ga                                                   CH.sub.2 C(F)CHBr         Ga                                                   CH.sub.2 C(I)CH.sub.2     Ga                                                   CH.sub.2 C(Cl)CCl.sub.2   Ga                                                   CH.sub.2 C(F)C(Cl)CF.sub.3                                                                               Ga                                                   CH.sub.2 CHC(F)CF.sub.2 Cl                                                                               Ga                                                   CH.sub.2 C(Br)CH.sub.2    Ga                                                   CH.sub.2 NHSO.sub.2 Me    Gb                                                   CH.sub.2 CH.sub.2 NHSO.sub.2 Me                                                                          Gb                                                   CH.sub.2 NHCOMe           Gb                                                   CH.sub.2 CH.sub.2 NHCOMe  Gb                                                   ______________________________________                                    

                  TABLE 2B                                                         ______________________________________                                          ##STR354##                                                                     ##STR355##                                                                     ##STR356##                                                                     ##STR357##                                                                     ##STR358##                                                                     ##STR359##                                                                     ##STR360##                                                                     ##STR361##                                                                     ##STR362##                                                                     ##STR363##                                                                     ##STR364##                                                                     ##STR365##                                                                     ##STR366##                                                                     ##STR367##                                                                     ##STR368##                                                                    ______________________________________                                         R.sup.m                   Gn                                                   ______________________________________                                         Me                        Ga                                                   Et                        Ga                                                   Pr-n                      Ga                                                   Pr-iso                    Ga                                                   Bu-n                      Ga                                                   Bu-iso                    Gb                                                   Pen-n                     Gb                                                   Hex-n                     Gb                                                   CH.sub.2 Prcyc            Ga                                                   CH.sub.2 CH.sub.2 Prcyc   Ga                                                   CH.sub.2 CHCH.sub.2       Ga                                                   CH.sub.2 CHCHMe           Ga                                                   CH.sub.2 CCH              Ga                                                   CH.sub.2 CCMe             Ga                                                   CH.sub.2 OMe              Ga                                                   CH.sub.2 OEt              Ga                                                   CH.sub.2 CH.sub.2 OMe     Ga                                                   CH.sub.2 CH.sub.2 OEt     Ga                                                   CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                            Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                   Ga                                                   CH.sub.2 OCH.sub.2 CCH    Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                          Ga                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                              Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                     Ga                                                   CH.sub.2 SMe              Ga                                                   CH.sub.2 SEt              Ga                                                   CH.sub.2 CH.sub.2 SMe     Ga                                                   CH.sub.2 CH.sub.2 SEt     Ga                                                   CH.sub.2 SO.sub.2 Me      Ga                                                   CH.sub.2 SO.sub.2 Et      Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                            Ga                                                   CH.sub.2 CH.sub.2 F       Ga                                                   CH.sub.2 CF.sub.3         Ga                                                   CH.sub.2 CN               Ga                                                   CH.sub.2 CH.sub.2 CN      Ga                                                   CHMeCN                    Ga                                                   CH.sub.2 CHCHCN           Ga                                                   CH.sub.2 NO.sub.2         Ga                                                   CH.sub.2 CH.sub.2 NO.sub.2                                                                               Ga                                                   CH.sub.2 CO.sub.2 Me      Gb                                                   CH.sub.2 CO.sub.2 Et      Gb                                                   CHMeCO.sub.2 Me           Gb                                                   CHMeCO.sub.2 Et           Gb                                                   CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                            Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                            Ga                                                   CH.sub.2 CHCHCO.sub.2 Me  Ga                                                   CH.sub.2 CHCHCO.sub.2 Et  Ga                                                   CHMeCHCHCO.sub.2 Me       Ga                                                   CH.sub.2 COMe             Ga                                                   CH.sub.2 COEt             Ga                                                   CH.sub.2 COPr-n           Gb                                                   CH.sub.2 COCF.sub.3       Ga                                                   CH.sub.2 COCHCH.sub.2     Ga                                                   CH.sub.2 COCHCHMe         Ga                                                   CH.sub.2 COCH.sub.2 OMe   Ga                                                   CH.sub.2 COCH.sub.2 OEt   Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                         Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                         Ga                                                   CH.sub.2 COCH.sub.2 SMe   Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                         Ga                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                          Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                 Ga                                                   CH.sub.2 CHCHCOMe         Ga                                                   CHMeCHCHCOMe              Ga                                                   CH.sub.2 SO.sub.2 NHMe    Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                          Gb                                                   CH.sub.2 SO.sub.2 NHOMe   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                         Gb                                                   CH.sub.2 SO.sub.2 NMe.sub.2                                                                              Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                     Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Me                                                                               Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                      Ga                                                   CH.sub.2 CONHMe           Gb                                                   CH.sub.2 CH.sub.2 CONHMe  Gb                                                   CH.sub.2 CONMe.sub.2      Ga                                                   CH.sub.2 CH.sub.2 CONMe.sub.2                                                                            Ga                                                   CH.sub.2 CONHOMe          Gb                                                   CH.sub.2 CH.sub.2 CONHOMe Gb                                                   CH.sub.2 CON(OMe)Me       Ga                                                   CH.sub.2 CH.sub.2 CON(OMe)Me                                                                             Ga                                                   CH.sub.2 NHMe             Gb                                                   CH.sub.2 CH.sub.2 NHMe    Gb                                                   CH.sub.2 NHOMe            Gb                                                   CH.sub.2 CH.sub.2 NHOMe   Gb                                                   CH.sub.2 NMe.sub.2        Ga                                                   CH.sub.2 CH.sub.2 NMe.sub.2                                                                              Ga                                                   CH.sub.2 N(OMe)Me         Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Me                                                                               Ga                                                   CH.sub.2 NMeCOMe          Ga                                                   CH.sub.2 CH.sub.2 NMeCOMe Ga                                                   CH.sub.2 N(OMe)COMe       Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COMe                                                                             Ga                                                   CH.sub.2 NMeSO.sub.2 Me   Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                         Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Me                                                                               Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                      Ga                                                   CH.sub.2 Ph               Gb                                                   CH.sub.2 CH.sub.2 Ph      Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                            Gb                                                   CHMePh                    Gb                                                   CH.sub.2 CHCHPh           Gb                                                   CHMeCHCHPh                Gb                                                   CH.sub.2 CH.sub.2 OPh     Gb                                                   CH.sub.2 OPh              Gb                                                   CH.sub.2 CH.sub.2 SPh     Gb                                                   CH.sub.2 SPh              Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                            Gb                                                   CH.sub.2 COPh             Gb                                                   CH.sub.2 CH.sub.2 COPh    Gb                                                   CH.sub.2 COCH.sub.2 Ph    Gb                                                   CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                          Gb                                                   Ph                        Ga                                                   ______________________________________                                    

                  TABLE 2C                                                         ______________________________________                                          ##STR369##                                                                     ##STR370##                                                                     ##STR371##                                                                     ##STR372##                                                                     ##STR373##                                                                     ##STR374##                                                                     ##STR375##                                                                     ##STR376##                                                                     ##STR377##                                                                     ##STR378##                                                                     ##STR379##                                                                     ##STR380##                                                                     ##STR381##                                                                     ##STR382##                                                                     ##STR383##                                                                     ##STR384##                                                                     ##STR385##                                                                     ##STR386##                                                                     ##STR387##                                                                     ##STR388##                                                                     ##STR389##                                                                     ##STR390##                                                                     ##STR391##                                                                     ##STR392##                                                                     ##STR393##                                                                     ##STR394##                                                                     ##STR395##                                                                     ##STR396##                                                                     ##STR397##                                                                     ##STR398##                                                                     ##STR399##                                                                     ##STR400##                                                                     ##STR401##                                                                     ##STR402##                                                                     ##STR403##                                                                     ##STR404##                                                                     ##STR405##                                                                     ##STR406##                                                                     ##STR407##                                                                     ##STR408##                                                                     ##STR409##                                                                     ##STR410##                                                                     ##STR411##                                                                     ##STR412##                                                                     ##STR413##                                                                     ##STR414##                                                                     ##STR415##                                                                     ##STR416##                                                                     ##STR417##                                                                     ##STR418##                                                                     ##STR419##                                                                     ##STR420##                                                                     ##STR421##                                                                     ##STR422##                                                                     ##STR423##                                                                     ##STR424##                                                                     ##STR425##                                                                     ##STR426##                                                                     ##STR427##                                                                     ##STR428##                                                                     ##STR429##                                                                     ##STR430##                                                                     ##STR431##                                                                     ##STR432##                                                                     ##STR433##                                                                     ##STR434##                                                                     ##STR435##                                                                     ##STR436##                                                                     ##STR437##                                                                     ##STR438##                                                                     ##STR439##                                                                     ##STR440##                                                                     ##STR441##                                                                     ##STR442##                                                                     ##STR443##                                                                     ##STR444##                                                                     ##STR445##                                                                     ##STR446##                                                                     ##STR447##                                                                     ##STR448##                                                                     ##STR449##                                                                     ##STR450##                                                                     ##STR451##                                                                     ##STR452##                                                                     ##STR453##                                                                     ##STR454##                                                                     ##STR455##                                                                     ##STR456##                                                                     ##STR457##                                                                     ##STR458##                                                                     ##STR459##                                                                     ##STR460##                                                                     ##STR461##                                                                    ______________________________________                                                R.sup.c1    Gn                                                          ______________________________________                                                Me          Ga                                                                 Et          Ga                                                                 Pr-n        Ga                                                                 Proiso      Gb                                                                 Bu-n        Ga                                                                 Bu-iso      Ga                                                                 Pen-n       Gb                                                                 CH.sub.2 Prcyc                                                                             Ga                                                                 CH.sub.2 CH.sub.2 Prcyc                                                                    Gb                                                                 CH.sub.2 CHCH.sub.2                                                                        Ga                                                                 CH.sub.2 CHCHMe                                                                            Ga                                                                 CH.sub.2 CCH                                                                               Ga                                                                 CH.sub.2 CCMe                                                                              Ga                                                                 CH.sub.2 CH.sub.2 OMe                                                                      Ga                                                                 CH.sub.2 OMe                                                                               Ga                                                                 CH.sub.2 CH.sub.2 SMe                                                                      Ga                                                                 CH.sub.2 SMe                                                                               Ga                                                                 CH.sub.2 SO.sub.2 Me                                                                       Ga                                                                 CH.sub.2 CH.sub.2 SO.sub.2 Me                                                              Ga                                                                 CH.sub.2 CF.sub.3                                                                          Ga                                                                 CH.sub.2 CN Ga                                                                 CH.sub.2 CH.sub.2 CN                                                                       Ga                                                                 CH.sub.2 NO.sub.2                                                                          Ga                                                                 CH.sub.2 CH.sub.2 NO.sub.2                                                                 Ga                                                                 CH.sub.2 COMe                                                                              Ga                                                                 CH.sub.2 COEt                                                                              Ga                                                                 CH.sub.2 COCHCH.sub.2                                                                      Ga                                                                 CH.sub.2 CHCHCOMe                                                                          Ga                                                                 CH.sub.2 CONMe.sub.2                                                                       Ga                                                                 Ph          Ga                                                          ______________________________________                                    

                  TABLE 3                                                          ______________________________________                                          ##STR462##                                                                     ##STR463##                                                                     ##STR464##                                                                     ##STR465##                                                                     ##STR466##                                                                     ##STR467##                                                                     ##STR468##                                                                     ##STR469##                                                                     ##STR470##                                                                     ##STR471##                                                                     ##STR472##                                                                     ##STR473##                                                                     ##STR474##                                                                     ##STR475##                                                                     ##STR476##                                                                     ##STR477##                                                                     ##STR478##                                                                     ##STR479##                                                                     ##STR480##                                                                     ##STR481##                                                                     ##STR482##                                                                     ##STR483##                                                                     ##STR484##                                                                     ##STR485##                                                                     ##STR486##                                                                     ##STR487##                                                                     ##STR488##                                                                     ##STR489##                                                                     ##STR490##                                                                     ##STR491##                                                                     ##STR492##                                                                     ##STR493##                                                                     ##STR494##                                                                     ##STR495##                                                                     ##STR496##                                                                     ##STR497##                                                                     ##STR498##                                                                     ##STR499##                                                                     ##STR500##                                                                     ##STR501##                                                                     ##STR502##                                                                     ##STR503##                                                                     ##STR504##                                                                     ##STR505##                                                                     ##STR506##                                                                     ##STR507##                                                                     ##STR508##                                                                     ##STR509##                                                                     ##STR510##                                                                     ##STR511##                                                                     ##STR512##                                                                     ##STR513##                                                                     ##STR514##                                                                     ##STR515##                                                                     ##STR516##                                                                     ##STR517##                                                                     ##STR518##                                                                     ##STR519##                                                                     ##STR520##                                                                     ##STR521##                                                                    ______________________________________                                                R.sup.n     Gn                                                          ______________________________________                                                Me          Ga                                                                 Et          Ga                                                                 Pr-n        Ga                                                                 Pr-iso      Gb                                                                 Bu-n        Gb                                                                 Pen-n       Gb                                                                 Hex-n       Gb                                                                 CH.sub.2 CHCH.sub.2                                                                        Ga                                                                 CH.sub.2 CHCHMe                                                                            Ga                                                                 CH.sub.2 CHCMe.sub.2                                                                       Gb                                                                 CHMeCHCH.sub.2                                                                             Gb                                                                 CH.sub.2 C CH                                                                              Ga                                                                 CH.sub.2 C CMe                                                                             Ga                                                                 CHMeC CH    Gb                                                                 CH.sub.2 SMe                                                                               Ga                                                                 CH.sub.2 SEt                                                                               Ga                                                                 CH.sub.2 SPr-n                                                                             Gb                                                                 CH.sub.2 CH.sub.2 SMe                                                                      Ga                                                                 CH.sub.2 CH.sub.2 SEt                                                                      Ga                                                                 CH.sub.2 SOMe                                                                              Gb                                                                 CH.sub.2 SOEt                                                                              Gb                                                                 CH.sub.2 CH.sub.2 SOMe                                                                     Gb                                                                 CH.sub.2 CH.sub.2 SOEt                                                                     Gb                                                                 CH.sub.2 SO.sub.2 Me                                                                       Ga                                                                 CH.sub.2 SO.sub.2 Et                                                                       Ga                                                                 CH.sub.2 SO.sub.2 Pr-n                                                                     Gb                                                                 CH.sub.2 CH.sub.2 SO.sub.2 Me                                                              Ga                                                                 CH.sub.2 CH.sub.2 SO.sub.2 Et                                                              Ga                                                                 CH.sub.2 OMe                                                                               Ga                                                                 CH.sub.2 OEt                                                                               Ga                                                                 CH.sub.2 OPr-n                                                                             Gb                                                                 CH.sub.2 CH.sub.2 OMe                                                                      Ga                                                                 CH.sub.2 CH.sub.2 OEt                                                                      Ga                                                                 CH.sub.2 CH.sub.2 OPr-n                                                                    Ga                                                                 CH.sub.2 CO.sub.2 Me                                                                       Ga                                                                 CH.sub.2 CO.sub.2 Et                                                                       Ga                                                                 CHMeCO.sub.2 Me                                                                            Ga                                                                 CHMeCO.sub.2 Et                                                                            Ga                                                                 CH.sub.2 COMe                                                                              Ga                                                                 CH.sub.2 COEt                                                                              Ga                                                                 CH.sub.2 COPr-n                                                                            Gb                                                                 CH.sub.2 CH.sub.2 COMe                                                                     Ga                                                                 CH.sub.2 CH.sub.2 COEt                                                                     Ga                                                                 CH.sub.2 CN Ga                                                                 CH.sub.2 CH.sub.2 CN                                                                       Ga                                                                 CH.sub.2 CH.sub.2 CH.sub.2 CN                                                              Ga                                                                 Ph          Ga                                                                 CH.sub.2 Ph Ga                                                                 CH.sub.2 CH.sub.2 Ph                                                                       Ga                                                                 CHMePh      Ga                                                          ______________________________________                                    

                  TABLE 4A                                                         ______________________________________                                          ##STR522##                                                                     ##STR523##                                                                     ##STR524##                                                                     ##STR525##                                                                     ##STR526##                                                                     ##STR527##                                                                     ##STR528##                                                                     ##STR529##                                                                     ##STR530##                                                                     ##STR531##                                                                     ##STR532##                                                                     ##STR533##                                                                     ##STR534##                                                                     ##STR535##                                                                     ##STR536##                                                                     ##STR537##                                                                     ##STR538##                                                                     ##STR539##                                                                     ##STR540##                                                                     ##STR541##                                                                    ______________________________________                                         R.sup.z1             Gn                                                        ______________________________________                                         Me                   Ga                                                        Et                   Ga                                                        Pr-n                 Ga                                                        Priso                Ga                                                        Bu-n                 Ga                                                        Bu-iso               Ga                                                        Bu-sec               Gb                                                        Bu-tert              Gb                                                        Pen-n                Ga                                                        Hex-n                Gb                                                        Hep-n                Gb                                                        Prcyc                Ga                                                        Hexcyc               Ga                                                        CH.sub.2 Prcyc       Ga                                                        CH.sub.2 CH.sub.2 Prcyc                                                                             Ga                                                        CH.sub.2 Bu-cyc      Gb                                                        CH.sub.2 Pen-cyc     Gc                                                        Hexen-cyc            Gb                                                        CH.sub.2 Penten-cyc  Gb                                                        CH.sub.2 CHCH.sub.2  Ga                                                        CH.sub.2 CHCHMe      Ga                                                        CH.sub.2 CHCHEt      Ga                                                        CH.sub.2 CHCMe.sub.2 Gb                                                        CH.sub.2 CMeCH.sub.2 Gb                                                        CH.sub.2 CMeCHCHMe   Gc                                                        CH.sub.2 CH.sub.2 CHCH.sub.2                                                                        Gb                                                        CH.sub.2 CH.sub.2 CHCHMe                                                                            Gb                                                        CH.sub.2 CCH         Ga                                                        CH.sub.2 CCMe        Ga                                                        CH.sub.2 CCEt        Ga                                                        CH.sub.2 CH.sub.2 CCH                                                                               Gb                                                        CH.sub.2 CH.sub.2 CCMe                                                                              Gb                                                        CHMeCCH              Gb                                                        CHMeCCMe             Gc                                                        CH.sub.2 OMe         Ga                                                        CH.sub.2 OEt         Ga                                                        CH.sub.2 OPr-n       Gb                                                        CH.sub.2 CH.sub.2 OMe                                                                               Ga                                                        CH.sub.2 CH.sub.2 OEt                                                                               Ga                                                        CH.sub.2 CH.sub.2 OPr-n                                                                             Gb                                                        CH.sub.2 CHMeOMe     Gb                                                        CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                      Ga                                                        CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                      Ga                                                        CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                       Ga                                                        CH.sub.2 OCH.sub.2 CHCHMe                                                                           Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                              Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                  Ga                                                        CH.sub.2 OCH.sub.2 CCH                                                                              Ga                                                        CH.sub.2 OCH.sub.2 CCMe                                                                             Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                     Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                    Ga                                                        CH.sub.2 OCHF.sub.2  Ga                                                        CH.sub.2 OCF.sub.3   Ga                                                        CH.sub.2 CH.sub.2 OCHF.sub.2                                                                        Ga                                                        CH.sub.2 CH.sub.2 OCF.sub.3                                                                         Ga                                                        CH.sub.2 OCH.sub.2 CF.sub.3                                                                         Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                Ga                                                        CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                       Ga                                                        CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                      Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                              Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                             Ga                                                        CH.sub.2 OCH.sub.2 CHCHCl                                                                           Gb                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                  Gb                                                        CH.sub.2 OCH.sub.2 CHCHBr                                                                           Gb                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                  Gb                                                        CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                       Gb                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                              Gb                                                        CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                     Gb                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                            Gb                                                        CH.sub.2 OCH.sub.2 CCI                                                                              Gb                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                     Gb                                                        CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                       Gb                                                        CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                              Gb                                                        CH.sub.2 SMe         Ga                                                        CH.sub.2 SEt         Ga                                                        CH.sub.2 SPr-n       Gb                                                        CH.sub.2 CH.sub.2 SMe                                                                               Ga                                                        CH.sub.2 CH.sub.2 SEt                                                                               Ga                                                        CH.sub.2 CH.sub.2 SPr-n                                                                             Gb                                                        CH.sub.2 SOMe        Gb                                                        CH.sub.2 SOEt        Gb                                                        CH.sub.2 CH.sub.2 SOMe                                                                              Gb                                                        CH.sub.2 CH.sub.2 SOEt                                                                              Gb                                                        CH.sub.2 SO.sub.2 Me Ga                                                        CH.sub.2 SO.sub.2 Et Ga                                                        CH.sub.2 SO.sub.2 Pr-n                                                                              Gb                                                        CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                       Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                       Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                     Gb                                                        CH.sub.2 CH.sub.2 F  Ga                                                        CH.sub.2 CHF.sub.2   Ga                                                        CH.sub.2 CF.sub.3    Ga                                                        CH.sub.2 CH.sub.2 Cl Ga                                                        CH.sub.2 CH.sub.2 Br Ga                                                        CH.sub.2 CH.sub.2 CF.sub.3                                                                          Ga                                                        CH.sub.2 CF.sub.2 CF.sub.3                                                                          Ga                                                        CH.sub.2 CHCHCl      Gb                                                        CH.sub.2 CHCHBr      Gb                                                        CH.sub.2 CHCF.sub.2  Gb                                                        CH.sub.2 CHCHCF.sub.3                                                                               Gb                                                        CH.sub.2 CCI         Gb                                                        CH.sub.2 CCCF.sub.3  Gb                                                        CH.sub.2 CN          Ga                                                        CH.sub.2 CH.sub.2 CN Ga                                                        CHMeCN               Ga                                                        CH.sub.2 CHCHCN      Ga                                                        CH(CN)CCH            Gb                                                        CH.sub.2 NO.sub.2    Ga                                                        CH.sub.2 CH.sub.2 NO.sub.2                                                                          Ga                                                        CH.sub.2 CHCHNO.sub.2                                                                               Gb                                                        CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                     Gc                                                        CH.sub.2 CH(NO.sub.2)CCH                                                                            Gc                                                        CH.sub.2 CO.sub.2 Me Gb                                                        CH.sub.2 CO.sub.2 Et Gb                                                        CH.sub.2 CO.sub.2 Pr-n                                                                              Gb                                                        CHMeCO.sub.2 Me      Gb                                                        CHMeCO.sub.2 Et      Gb                                                        CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                       Ga                                                        CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                       Ga                                                        CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                              Gb                                                        CH.sub.2 CHCHCO.sub.2 Me                                                                            Ga                                                        CH.sub.2 CHCHCO.sub.2 Et                                                                            Ga                                                        CHMeCHCHCO.sub.2 Me  Ga                                                        CHMeCHCHCO.sub.2 Et  Ga                                                        CH.sub.2 CCCO.sub.2 Me                                                                              Ga                                                        CH.sub.2 CCCO.sub.2 Et                                                                              Ga                                                        CH.sub.2 COMe        Ga                                                        CH.sub.2 COEt        Ga                                                        CH.sub.2 COPr-n      Gb                                                        CH.sub.2 CH.sub.2 COMe                                                                              Ga                                                        CH.sub.2 CH.sub.2 COEt                                                                              Ga                                                        CH.sub.2 COCF.sub.3  Ga                                                        CH.sub.2 CH.sub.2 COCF.sub.3                                                                        Ga                                                        CH.sub.2 COCH.sub.2 CF.sub.3                                                                        Gb                                                        CH.sub.2 COCH.sub.2 F                                                                               Gb                                                        CH.sub.2 COCHCH.sub.2                                                                               Ga                                                        CH.sub.2 COCHCHMe    Ga                                                        CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                      Gb                                                        CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                      Gb                                                        CH.sub.2 CH.sub.2 COCHCHMe                                                                          Gb                                                        CH.sub.2 COCCH       Ga                                                        CH.sub.2 COCCMe      Ga                                                        CH.sub.2 COCH.sub.2 OMe                                                                             Ga                                                        CH.sub.2 COCH.sub.2 OEt                                                                             Ga                                                        CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                    Ga                                                        CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                    Ga                                                        CH.sub.2 COCH.sub.2 SMe                                                                             Ga                                                        CH.sub.2 COCH.sub.2 SEt                                                                             Ga                                                        CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                    Ga                                                        CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                    Ga                                                        CH.sub.2 COCH.sub.2 SOMe                                                                            Gb                                                        CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                   Gb                                                        CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                     Ga                                                        CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                     Ga                                                        CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                            Ga                                                        CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                            Ga                                                        CH.sub.2 CHCHCOMe    Ga                                                        CH.sub.2 CHCHCOEt    Ga                                                        CHMeCHCHCOMe         Ga                                                        CHMeCHCHCOEt         Ga                                                        CH.sub.2 CCCOMe      Ga                                                        CH.sub.2 CCCOEt      Ga                                                        CH.sub.2 SO.sub.2 NHMe                                                                              Ga                                                        CH.sub.2 SO.sub.2 NHEt                                                                              Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                     Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                     Ga                                                        CH.sub.2 SO.sub.2 NHOMe                                                                             Ga                                                        CH.sub.2 SO.sub.2 NHOEt                                                                             Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                    Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                    Ga                                                        CH.sub.2 SO.sub.2 NMe.sub.2                                                                         Ga                                                        CH.sub.2 SO.sub.2 NMeEt                                                                             Ga                                                        CH.sub.2 SO.sub.2 NEt.sub.2                                                                         Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                    Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                Ga                                                        CH.sub.2 SO.sub.2 N(OMe)Me                                                                          Ga                                                        CH.sub.2 SO.sub.2 N(OMe)Et                                                                          Ga                                                        CH.sub.2 SO.sub.2 N(OEt)Me                                                                          Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                 Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                 Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                 Ga                                                        CH.sub.2 CONHMe      Ga                                                        CH.sub.2 CONHEt      Ga                                                        CH.sub.2 CONHPr-n    Gb                                                        CH.sub.2 CH.sub.2 CONHMe                                                                            Ga                                                        CH.sub.2 CH.sub.2 CONHEt                                                                            Ga                                                        CH.sub.2 CH.sub.2 CONHPr-n                                                                          Gb                                                        CH.sub.2 CONMe.sub.2 Ga                                                        CH.sub.2 CONMeEt     Ga                                                        CH.sub.2 CONEt.sub.2 Ga                                                        CH.sub.2 CONHOMe     Ga                                                        CH.sub.2 CONHOEt     Ga                                                        CH.sub.2 CONHOPr-n   Gb                                                        CH.sub.2 CON(OMe)Me  Ga                                                        CH.sub.2 CON(OMe)Et  Ga                                                        CH.sub.2 CON(OEt)Me  Ga                                                        CH.sub.2 CON(OEt)Et  Ga                                                        CH.sub.2 NHMe        Ga                                                        CH.sub.2 NHEt        Ga                                                        CH.sub.2 NHPr-n      Gb                                                        CH.sub.2 CH.sub.2 NHMe                                                                              Ga                                                        CH.sub.2 CH.sub.2 NHEt                                                                              Ga                                                        CH.sub.2 CH.sub.2 NHPr-n                                                                            Gb                                                        CH.sub.2 NHOMe       Ga                                                        CH.sub.2 NHOEt       Ga                                                        CH.sub.2 CH.sub.2 NHOMe                                                                             Ga                                                        CH.sub.2 CH.sub.2 NHOEt                                                                             Ga                                                        CH.sub.2 NMe.sub.2   Ga                                                        CH.sub.2 NMeEt       Ga                                                        CH.sub.2 CH.sub.2 NMe.sub.2                                                                         Ga                                                        CH.sub.2 CH.sub.2 NMeEt                                                                             Ga                                                        CH.sub.2 N(OMe)Me    Ga                                                        CH.sub.2 N(OMe)Et    Ga                                                        CH.sub.2 N(OEt)Me    Ga                                                        CH.sub.2 CH.sub.2 N(OMe)Me                                                                          Ga                                                        CH.sub.2 CH.sub.2 N(OMe)Et                                                                          Ga                                                        CH.sub.2 CH.sub.2 N(OEt)Me                                                                          Ga                                                        CH.sub.2 NMeCOMe     Ga                                                        CH.sub.2 NEtCOMe     Ga                                                        CH.sub.2 NMeCOEt     Ga                                                        CH.sub.2 CH.sub.2 NMeCOMe                                                                           Ga                                                        CH.sub.2 CH.sub.2 NEtCOMe                                                                           Ga                                                        CH.sub.2 CH.sub.2 NMeCOEt                                                                           Ga                                                        CH.sub.2 N(OMe)COMe  Ga                                                        CH.sub.2 N(OEt)COMe  Ga                                                        CH.sub.2 N(OMe)COEt  Ga                                                        CH.sub.2 CH.sub.2 N(OMe)COMe                                                                        Ga                                                        CH.sub.2 CH.sub.2 N(OEt)COMe                                                                        Ga                                                        CH.sub.2 CH.sub.2 N(OMe)COEt                                                                        Ga                                                        CH.sub.2 NMeSO.sub.2 Me                                                                             Ga                                                        CH.sub.2 NEtSO.sub.2 Me                                                                             Ga                                                        CH.sub.2 NMeSO.sub.2 Et                                                                             Ga                                                        CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                    Ga                                                        CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                    Ga                                                        CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                    Ga                                                        CH.sub.2 N(OMe)SO.sub.2 Me                                                                          Ga                                                        CH.sub.2 N(OEt)SO.sub.2 Me                                                                          Ga                                                        CH.sub.2 N(OMe)SO.sub.2 Et                                                                          Ga                                                        CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                 Ga                                                        CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                 Ga                                                        CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                 Ga                                                        CH.sub.2 Ph          Gb                                                        CH.sub.2 CH.sub.2 Ph Gb                                                        CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                       Gb                                                        CHMePh               Gb                                                        CH.sub.2 CHCHPh      Ga                                                        CHMeCHCHPh           Ga                                                        CH.sub.2 CCPh        Ga                                                        CHMeCCPh             Ga                                                        CH.sub.2 CH.sub.2 OPh                                                                               Ga                                                        CH.sub.2 OPh         Ga                                                        CH.sub.2 CH.sub.2 SPh                                                                               Ga                                                        CH.sub.2 SPh         Ga                                                        CH.sub.2 CH.sub.2 SOPh                                                                              Gb                                                        CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                       Ga                                                        CH.sub.2 OCH.sub.2 Ph                                                                               Ga                                                        CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                      Ga                                                        CH.sub.2 SCH.sub.2 Ph                                                                               Ga                                                        CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                      Ga                                                        CH.sub.2 SOCH.sub.2 Ph                                                                              Gb                                                        CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                     Gb                                                        CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                       Ga                                                        CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                              Ga                                                        CH.sub.2 COPh        Ga                                                        CH.sub.2 CH.sub.2 COPh                                                                              Ga                                                        CHMeCOPh             Ga                                                        CH.sub.2 COCH.sub.2 Ph                                                                              Gb                                                        CHMeCOCH.sub.2 Ph    Gb                                                        CH.sub.2 CH.sub.2 CH.sub.2 F                                                                        Ga                                                        CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                       Ga                                                        ______________________________________                                    

                  TABLE 4B                                                         ______________________________________                                          ##STR542##                                                                     ##STR543##                                                                     ##STR544##                                                                     ##STR545##                                                                     ##STR546##                                                                     ##STR547##                                                                     ##STR548##                                                                     ##STR549##                                                                     ##STR550##                                                                     ##STR551##                                                                     ##STR552##                                                                     ##STR553##                                                                     ##STR554##                                                                     ##STR555##                                                                     ##STR556##                                                                     ##STR557##                                                                     ##STR558##                                                                    ______________________________________                                         R.sup.z1            Gn                                                         ______________________________________                                         Me                  Ga                                                         Et                  Ga                                                         Pr-n                Ga                                                         Priso               Ga                                                         Bu-n                Ga                                                         Bu-iso              Gb                                                         Pen-n               Gb                                                         Hex-n               Gb                                                         CH.sub.2 Prcyc      Ga                                                         CH.sub.2 CH.sub.2 Prcyc                                                                            Ga                                                         CH.sub.2 CHCH.sub.2 Ga                                                         CH.sub.2 CHCHMe     Ga                                                         CH.sub.2 CHCH       Ga                                                         CH.sub.2 CCMe       Ga                                                         CH.sub.2 OMe        Ga                                                         CH.sub.2 OEt        Ga                                                         CH.sub.2 CH.sub.2 OMe                                                                              Ga                                                         CH.sub.2 CH.sub.2 OEt                                                                              Ga                                                         CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                      Ga                                                         CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                             Ga                                                         CH.sub.2 OCH.sub.2 CCH                                                                             Ga                                                         CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                    Ga                                                         CH.sub.2 OCH.sub.2 CF.sub.3                                                                        Ga                                                         CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                               Ga                                                         CH.sub.2 SMe        Ga                                                         CH.sub.2 SEt        Ga                                                         CH.sub.2 CH.sub.2 SMe                                                                              Ga                                                         CH.sub.2 CH.sub.2 SEt                                                                              Ga                                                         CH.sub.2 SO.sub.2 Me                                                                               Ga                                                         CH.sub.2 SO.sub.2 Et                                                                               Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                      Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                      Ga                                                         CH.sub.2 CH.sub.2 F Ga                                                         CH.sub.2 CF.sub.3   Ga                                                         CH.sub.2 CN         Ga                                                         CH.sub.2 CH.sub.2 CN                                                                               Ga                                                         CHMeCN              Ga                                                         CH.sub.2 CHCHCN     Ga                                                         CH.sub.2 NO.sub.2   Ga                                                         CH.sub.2 CH.sub.2 NO.sub.2                                                                         Ga                                                         CH.sub.2 CO.sub.2 Me                                                                               Gb                                                         CH.sub.2 CO.sub.2 Et                                                                               Gb                                                         CHMeCO.sub.2 Me     Gb                                                         CHMeCO.sub.2 Et     Gb                                                         CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                      Ga                                                         CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                      Ga                                                         CH.sub.2 CHCHCO.sub.2 Me                                                                           Ga                                                         CH.sub.2 CHCHCO.sub.2 Et                                                                           Ga                                                         CHMeCHCHCO.sub.2 Me Ga                                                         CH.sub.2 COMe       Ga                                                         CH.sub.2 COEt       Ga                                                         CH.sub.2 COPr-n     Gb                                                         CH.sub.2 COCF.sub.3 Ga                                                         CH.sub.2 COCHCH.sub.2                                                                              Ga                                                         CH.sub.2 COCHCHMe   Ga                                                         CH.sub.2 COCH.sub.2 OMe                                                                            Ga                                                         CH.sub.2 COCH.sub.2 OEt                                                                            Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                   Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                   Ga                                                         CH.sub.2 COCH.sub.2 SMe                                                                            Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                   Ga                                                         CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                    Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                           Ga                                                         CH.sub.2 CHCHCOMe   Ga                                                         CHMeCHCHCOMe        Ga                                                         CH.sub.2 SO.sub.2 NHMe                                                                             Gb                                                         CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                    Gb                                                         CH.sub.2 SO.sub.2 NHOMe                                                                            Gb                                                         CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                   Gb                                                         CH.sub.2 SO.sub.2 NMe.sub.2                                                                        Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                               Ga                                                         CH.sub.2 SO.sub.2 N(OMe)Me                                                                         Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                Ga                                                         CH.sub.2 CONHMe     Gb                                                         CH.sub.2 CH.sub.2 CONHMe                                                                           Gb                                                         CH.sub.2 CONMe.sub.2                                                                               Ga                                                         CH.sub.2 CH.sub.2 CONMe.sub.2                                                                      Ga                                                         CH.sub.2 CONHOMe    Gb                                                         CH.sub.2 CH.sub.2 CONHOMe                                                                          Gb                                                         CH.sub.2 CON(OMe)Me Ga                                                         CH.sub.2 CH.sub.2 CON(OMe)Me                                                                       Ga                                                         CH.sub.2 NHMe       Gb                                                         CH.sub.2 CH.sub.2 NHMe                                                                             Gb                                                         CH.sub.2 NHOMe      Gb                                                         CH.sub.2 CH.sub.2 NHOMe                                                                            Gb                                                         CH.sub.2 NMe.sub.2  Ga                                                         CH.sub.2 CH.sub.2 NMe.sub.2                                                                        Ga                                                         CH.sub.2 N(OMe)Me   Ga                                                         CH.sub.2 CH.sub.2 N(OMe)Me                                                                         Ga                                                         CH.sub.2 NMeCOMe    Ga                                                         CH.sub.2 CH.sub.2 NMeCOMe                                                                          Ga                                                         CH.sub.2 N(OMe)COMe Ga                                                         CH.sub.2 CH.sub.2 N(OMe)COMe                                                                       Ga                                                         CH.sub.2 NMeSO.sub.2 Me                                                                            Ga                                                         CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                   Ga                                                         CH.sub.2 N(OMe)SO.sub.2 Me                                                                         Ga                                                         CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                Ga                                                         CH.sub.2 Ph         Gb                                                         CH.sub.2 CH.sub.2 Ph                                                                               Gb                                                         CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                      Gb                                                         CHMePh              Gb                                                         CH.sub.2 CHCHPh     Gb                                                         CHMeCHCHPh          Gb                                                         CH.sub.2 CH.sub.2 OPh                                                                              Gb                                                         CH.sub.2 OPh        Gb                                                         CH.sub.2 CH.sub.2 SPh                                                                              Gb                                                         CH.sub.2 SPh        Gb                                                         CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                      Gb                                                         CH.sub.2 COPh       Gb                                                         CH.sub.2 CH.sub.2 COPh                                                                             Gb                                                         CH.sub.2 COCH.sub.2 Ph                                                                             Gb                                                         CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                    Gb                                                         ______________________________________                                    

                  TABLE 4C                                                         ______________________________________                                          ##STR559##                                                                     ##STR560##                                                                     ##STR561##                                                                     ##STR562##                                                                     ##STR563##                                                                    ______________________________________                                                R.sup.z1    Gn                                                          ______________________________________                                                Me          Ga                                                                 Et          Ga                                                                 Pr-n        Ga                                                                 Proiso      Gb                                                                 Bu-n        Ga                                                                 Bu-iso      Ga                                                                 Pen-n       Gb                                                                 CH.sub.2 Prcyc                                                                             Ga                                                                 CH.sub.2 CH.sub.2 Prcyc                                                                    Gb                                                                 CH.sub.2 CHCH.sub.2                                                                        Ga                                                                 CH.sub.2 CHCHMe                                                                            Ga                                                                 CH.sub.2 CCH                                                                               Ga                                                                 CH.sub.2 CCMe                                                                              Ga                                                                 CH.sub.2 CH.sub.2 OMe                                                                      Ga                                                                 CH.sub.2 OMe                                                                               Ga                                                                 CH.sub.2 CH.sub.2 SMe                                                                      Ga                                                                 CH.sub.2 SMe                                                                               Ga                                                                 CH.sub.2 SO.sub.2 Me                                                                       Ga                                                                 CH.sub.2 CH.sub.2 SO.sub.2 Me                                                              Ga                                                                 CH.sub.2 CF.sub.3                                                                          Ga                                                                 CH.sub.2 CN Ga                                                                 CH.sub.2 CH.sub.2 CN                                                                       Ga                                                                 CH.sub.2 NO.sub.2                                                                          Ga                                                                 CH.sub.2 CH.sub.2 NO.sub.2                                                                 Ga                                                                 CH.sub.2 COMe                                                                              Ga                                                                 CH.sub.2 COEt                                                                              Ga                                                                 CH.sub.2 COCHCH.sub.2                                                                      Ga                                                                 CH.sub.2 CHCHCOMe                                                                          Ga                                                                 CH.sub.2 CONMe.sub.2                                                                       Ga                                                          ______________________________________                                    

                  TABLE 5                                                          ______________________________________                                          ##STR564##                                                                     ##STR565##                                                                     ##STR566##                                                                     ##STR567##                                                                     ##STR568##                                                                     ##STR569##                                                                     ##STR570##                                                                     ##STR571##                                                                     ##STR572##                                                                     ##STR573##                                                                     ##STR574##                                                                     ##STR575##                                                                     ##STR576##                                                                     ##STR577##                                                                     ##STR578##                                                                     ##STR579##                                                                     ##STR580##                                                                     ##STR581##                                                                     ##STR582##                                                                     ##STR583##                                                                     ##STR584##                                                                     ##STR585##                                                                     ##STR586##                                                                     ##STR587##                                                                     ##STR588##                                                                     ##STR589##                                                                     ##STR590##                                                                     ##STR591##                                                                     ##STR592##                                                                     ##STR593##                                                                     ##STR594##                                                                     ##STR595##                                                                     ##STR596##                                                                     ##STR597##                                                                     ##STR598##                                                                     ##STR599##                                                                     ##STR600##                                                                     ##STR601##                                                                     ##STR602##                                                                     ##STR603##                                                                     ##STR604##                                                                     ##STR605##                                                                     ##STR606##                                                                     ##STR607##                                                                     ##STR608##                                                                     ##STR609##                                                                     ##STR610##                                                                     ##STR611##                                                                     ##STR612##                                                                     ##STR613##                                                                     ##STR614##                                                                    ______________________________________                                         R.sup.m          L              Gn                                             ______________________________________                                         Me               Me             Ga                                             Me               Et             Gb                                             Et               Me             Ga                                             Et               Et             Gb                                             Pr-n             Me             Ga                                             Pr-n             Et             Gb                                             Pr-n             CH.sub.2 CHCH.sub.2                                                                           Gb                                             Pr-n             CH.sub.2 C CH  Gb                                             Bu-n             Me             Ga                                             Bu-n             Et             Gb                                             Bu-n             CH.sub.2 CHCH.sub.2                                                                           Gb                                             Bu-n             CH.sub.2 C CH  Gb                                             Pen-n            Me             Gb                                             CH.sub.2 CHCH.sub.2                                                                             Me             Ga                                             CH.sub.2 CHCH.sub.2                                                                             Et             Gb                                             CH.sub.2 CHCH.sub.2                                                                             CH.sub.2 CHCH.sub.2                                                                           Gb                                             CH.sub.2 CHCH.sub.2                                                                             CH.sub.2 C CH  Gb                                             CH.sub.2 C CH    Me             Gb                                             CH.sub.2 C CH    Et             Gb                                             CH.sub.2 C CH    CH.sub.2 CHCH.sub.2                                                                           Gb                                             CH.sub.2 C CH    CH.sub.2 C CH  Gb                                             CH.sub.2 CH.sub.2 OMe                                                                           Me             Gb                                             CH.sub.2 CH.sub.2 SMe                                                                           Me             Gb                                             CH.sub.2 SO.sub.2 Me                                                                            Me             Gb                                             CH.sub.2 CF.sub.3                                                                               Me             Gb                                             CH.sub.2 CF.sub.3                                                                               Et             Gb                                             CH.sub.2 CF.sub.3                                                                               CH.sub.2 CHCH.sub.2                                                                           Gb                                             CH.sub.2 CF.sub.3                                                                               CH.sub.2 C CH  Gb                                             CH.sub.2 CN      Me             Gb                                             CH.sub.2 COMe    Me             Gb                                             CH.sub.2 COMe    Et             Gb                                             CH.sub.2 COMe    CH.sub.2 CHCH.sub.2                                                                           Gb                                             CH.sub.2 COMe    CH.sub.2 C CH  Gb                                             CH.sub.2 COCHCH.sub.2                                                                           Me             Gb                                             CH.sub.2 CONMe.sub.2                                                                            Me             Gb                                             ______________________________________                                    

                  TABLE 6                                                          ______________________________________                                          ##STR615##                                                                     ##STR616##                                                                     ##STR617##                                                                     ##STR618##                                                                     ##STR619##                                                                     ##STR620##                                                                     ##STR621##                                                                     ##STR622##                                                                     ##STR623##                                                                     ##STR624##                                                                     ##STR625##                                                                     ##STR626##                                                                     ##STR627##                                                                     ##STR628##                                                                     ##STR629##                                                                     ##STR630##                                                                     ##STR631##                                                                     ##STR632##                                                                    ______________________________________                                         R.sup.c1         L             Gn                                              ______________________________________                                         Me               Me            Ga                                              Me               Et            Gb                                              Me               CH.sub.2 CHCH.sub.2                                                                          Gb                                              Me               CH.sub.2 C CH Gb                                              Et               Me            Ga                                              Et               Et            Gb                                              Et               CH.sub.2 CHCH.sub.2                                                                          Gb                                              Et               CH.sub.2 C CH Gb                                              Pr-n             Me            Ga                                              Pr-n             Et            Gb                                              Bu-n             Me            Ga                                              Bu-n             Et            Gb                                              Pen-n            Me            Gb                                              CH.sub.2 CHCH.sub.2                                                                             Me            Ga                                              CH.sub.2 CHCH.sub.2                                                                             Et            Gb                                              CH.sub.2 CHCH.sub.2                                                                             CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 CHCH.sub.2                                                                             CH.sub.2 C CH Gb                                              CH.sub.2 C CH    Me            Gb                                              CH.sub.2 C CH    Et            Gb                                              CH.sub.2 C CH    CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 C CH    CH.sub.2 C CH Gb                                              CH.sub.2 CH.sub.2 OMe                                                                           Me            Gb                                              CH.sub.2 CH.sub.2 SMe                                                                           Me            Gb                                              CH.sub.2 SO.sub.2 Me                                                                            Me            Gb                                              CH.sub.2 CF.sub.3                                                                               Me            Gb                                              CH.sub.2 CF.sub.3                                                                               Et            Gb                                              CH.sub.2 CF.sub.3                                                                               CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 CF.sub.3                                                                               CH.sub.2 C CH Gb                                              CH.sub.2 CN      Me            Gb                                              CH.sub.2 COMe    Me            Gb                                              CH.sub.2 COMe    Et            Gb                                              CH.sub.2 COMe    CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 COMe    CH.sub.2 C CH Gb                                              CH.sub.2 COCHCH.sub.2                                                                           Me            Gb                                              CH.sub.2 CONMe.sub.2                                                                            Me            Gb                                              Ph               Me            Gb                                              ______________________________________                                    

                  TABLE 7                                                          ______________________________________                                          ##STR633##                                                                     ##STR634##                                                                     ##STR635##                                                                     ##STR636##                                                                     ##STR637##                                                                     ##STR638##                                                                     ##STR639##                                                                     ##STR640##                                                                     ##STR641##                                                                     ##STR642##                                                                     ##STR643##                                                                     ##STR644##                                                                     ##STR645##                                                                     ##STR646##                                                                     ##STR647##                                                                     ##STR648##                                                                     ##STR649##                                                                     ##STR650##                                                                     ##STR651##                                                                     ##STR652##                                                                     ##STR653##                                                                     ##STR654##                                                                     ##STR655##                                                                     ##STR656##                                                                     ##STR657##                                                                     ##STR658##                                                                     ##STR659##                                                                    ______________________________________                                         R.sup.n          L              Gn                                             ______________________________________                                         Me               Me             Ga                                             Me               Et             Gb                                             Me               CH.sub.2 CHCH.sub.2                                                                           Gb                                             Me               CH.sub.2 C CH  Gb                                             Et               Me             Ga                                             Et               Et             Gb                                             Et               CH.sub.2 CHCH.sub.2                                                                           Gb                                             Et               CH.sub.2 C CH  Gb                                             Pr-n             Me             Ga                                             Pr-n             Et             Gb                                             Pr-n             CH.sub.2 CHCH.sub.2                                                                           Gb                                             Pr-n             CH.sub.2 C CH  Gb                                             CH.sub.2 CHCH.sub.2                                                                             Me             Gb                                             CH.sub.2 C CH    Me             Gb                                             CH.sub.2 SMe     Me             Gb                                             CH.sub.2 CH.sub.2 SMe                                                                           Me             Gb                                             CH.sub.2 SO.sub.2 Me                                                                            Me             Gb                                             CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                   Me             Gb                                             CH.sub.2 OMe     Me             Gb                                             CH.sub.2 CH.sub.2 OMe                                                                           Me             Gb                                             CH.sub.2 CO.sub.2 Me                                                                            Me             Gb                                             CH.sub.2 COMe    Me             Gb                                             CH.sub.2 CH.sub.2 COMe                                                                          Me             Gb                                             CH.sub.2 CN      Me             Gb                                             CH.sub.2 CH.sub.2 CN                                                                            Me             Gb                                             Ph               Me             Gb                                             CH.sub.2 Ph      Me             Gb                                             CH.sub.2 CH.sub.2 Ph                                                                            Me             Gb                                             CHMePh           Me             Gb                                             ______________________________________                                    

                  TABLE 8                                                          ______________________________________                                          ##STR660##                                                                     ##STR661##                                                                                      ##STR662##                                                    ##STR663##                                                                                      ##STR664##                                                    ##STR665##                                                                                      ##STR666##                                                    ##STR667##                                                                                      ##STR668##                                                    ##STR669##                                                                                      ##STR670##                                                    ##STR671##                                                                                      ##STR672##                                                    ##STR673##                                                                                      ##STR674##                                                    ##STR675##                                                                                      ##STR676##                                                    ##STR677##                                                                                      ##STR678##                                                    ##STR679##                                                                                      ##STR680##                                                    ##STR681##                                                                                      ##STR682##                                                    ##STR683##                                                                    ______________________________________                                         R.sup.g1        L               Gn                                             ______________________________________                                         Me              Me              Ga                                             Me              Et              Gb                                             Et              Me              Ga                                             Et              Et              Gb                                             Pr-n            Me              Ga                                             Pr-n            Et              Gb                                             Pr-n            CH.sub.2 CHCH.sub.2                                                                            Gb                                             Pr-n            CH.sub.2 CCH    Gb                                             Bu-n            Me              Ga                                             Bu-n            Et              Gb                                             Bu-n            CH.sub.2 CHCH.sub.2                                                                            Gb                                             Bu-n            CH.sub.2 CCH    Gb                                             Pen-n           Me              Gb                                             CH.sub.2 CHCH.sub.2                                                                            Me              Ga                                             CH.sub.2 CHCH.sub.2                                                                            Et              Gb                                             CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 CHCH.sub.2                                                                            Gb                                             CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 CCH    Gb                                             CH.sub.2 CCH    Me              Gb                                             CH.sub.2 CCH    Et              Gb                                             CH.sub.2 CCH    CH.sub.2 CHCH.sub.2                                                                            Gb                                             CH.sub.2 CCH    CH.sub.2 CCH    Gb                                             CH.sub.2 CH.sub.2 OMe                                                                          Me              Gb                                             CH.sub.2 CH.sub.2 SMe                                                                          Me              Gb                                             CH.sub.2 SO.sub.2 Me                                                                           Me              Gb                                             CH.sub.2 CF.sub.3                                                                              Me              Gb                                             CH.sub.2 CF.sub.3                                                                              Et              Gb                                             CH.sub.2 CF.sub.3                                                                              CH.sub.2 CHCH.sub.2                                                                            Gb                                             CH.sub.2 CF.sub.3                                                                              CH.sub.2 CCH    Gb                                             CH.sub.2 CN     Me              Gb                                             CH.sub.2 COMe   Me              Gb                                             CH.sub.2 COMe   Et              Gb                                             CH.sub.2 COMe   CH.sub.2 CHCH.sub.2                                                                            Gb                                             CH.sub.2 COMe   CH.sub.2 CCH    Gb                                             CH.sub.2 COCHCH.sub.2                                                                          Me              Gb                                             CH.sub.2 CONMe.sub.2                                                                           Me              Gb                                             ______________________________________                                    

                  TABLE 9                                                          ______________________________________                                          ##STR684##                                                                     ##STR685##                                                                     ##STR686##                                                                     ##STR687##                                                                     ##STR688##                                                                     ##STR689##                                                                     ##STR690##                                                                     ##STR691##                                                                     ##STR692##                                                                     ##STR693##                                                                    R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or                   ______________________________________                                         R.sup.f1.                                                                      R.sup.m                  Gn                                                    ______________________________________                                         Me                       Gc                                                    Et                       Gc                                                    Pr-n                     Gc                                                    Pr-iso                   Gc                                                    Bu-n                     Gc                                                    Bu-iso                   Gc                                                    Pen-n                    Gc                                                    CH.sub.2 Pr-cyc          Gc                                                    CH.sub.2 CH.sub.2 Py-cyc Gc                                                    CH.sub.2 CHCH.sub.2      Gc                                                    CH.sub.2 CHCHMe          Gc                                                    CH.sub.2 CCH             Gc                                                    CH.sub.2 CCMe            Gc                                                    CH.sub.2 CH.sub.2 OMe    Gc                                                    CH.sub.2 OMe             Gc                                                    CH.sub.2 CH.sub.2 SMe    Gc                                                    CH.sub.2 SMe             Gc                                                    CH.sub.2 SO.sub.2 Me     Gc                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Gc                                                    CH.sub.2 CF.sub.3        Gc                                                    CH.sub.2 CN              Gc                                                    CH.sub.2 CH.sub.2 CN     Gc                                                    CH.sub.2 NO.sub.2        Gc                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Gc                                                    CH.sub.2 COMe            Gc                                                    CH.sub.2 COEt            Gc                                                    CH.sub.2 COCHCH.sub.2    Gc                                                    CH.sub.2 CHCHCOMe        Gc                                                    CH.sub.2 CONMe.sub.2     Gc                                                    ______________________________________                                    

                  TABLE 10                                                         ______________________________________                                          ##STR694##                                                                     ##STR695##                                                                     ##STR696##                                                                     ##STR697##                                                                    ______________________________________                                         R.sup.c1                 Gn                                                    ______________________________________                                         Me                       Gc                                                    Et                       Gc                                                    Pr-n                     Gc                                                    Pr-iso                   Gc                                                    Bu-n                     Gc                                                    Bu-iso                   Gc                                                    Pen-n                    Gc                                                    CH.sub.2 Pr-cyc          Gc                                                    CH.sub.2 CH.sub.2 Py-cyc Gc                                                    CH.sub.2 CHCH.sub.2      Gc                                                    CH.sub.2 CHCHMe          Gc                                                    CH.sub.2 CCH             Gc                                                    CH.sub.2 CCMe            Gc                                                    CH.sub.2 CH.sub.2 OMe    Gc                                                    CH.sub.2 OMe             Gc                                                    CH.sub.2 CH.sub.2 SMe    Gc                                                    CH.sub.2 SMe             Gc                                                    CH.sub.2 SO.sub.2 Me     Gc                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Gc                                                    CH.sub.2 CF.sub.3        Gc                                                    CH.sub.2 CN              Gc                                                    CH.sub.2 CH.sub.2 CN     Gc                                                    CH.sub.2 NO.sub.2        Gc                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Gc                                                    CH.sub.2 COMe            Gc                                                    CH.sub.2 COEt            Gc                                                    CH.sub.2 COCHCH.sub.2    Gc                                                    CH.sub.2 CHCHCOMe        Gc                                                    CH.sub.2 CONMe.sub.2     Gc                                                    Ph                       Gc                                                    ______________________________________                                    

                  TABLE 11                                                         ______________________________________                                          ##STR698##                                                                     ##STR699##                                                                     ##STR700##                                                                     ##STR701##                                                                     ##STR702##                                                                    ______________________________________                                         R.sup.n represents R.sup.d6 or R.sup.f2.                                       ______________________________________                                                R.sup.n          Gn                                                     ______________________________________                                                Me               Gc                                                            Et               Gc                                                            Pr-n             Gc                                                            CH.sub.2 CHCH.sub.2                                                                             Gc                                                            CH.sub.2 CCH     Gc                                                            CH.sub.2 SMe     Gc                                                            CH.sub.2 CH.sub.2 SMe                                                                           Gc                                                            CH.sub.2 SO.sub.2 Me                                                                            Gc                                                            CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                   Gc                                                            CH.sub.2 OMe     Gc                                                            CH.sub.2 CH.sub.2 OMe                                                                           Gc                                                            CH.sub.2 CO.sub.2 Me                                                                            Gc                                                            CH.sub.2 COMe    Gc                                                            CH.sub.2 CH.sub.2 COMe                                                                          Gc                                                            CH.sub.2 CN      Gc                                                            CH.sub.2 CH.sub.2 CN                                                                            Gc                                                            Ph               Gc                                                            CH.sub.2 Ph      Gc                                                     ______________________________________                                    

                  TABLE 12                                                         ______________________________________                                          ##STR703##                                                                     ##STR704##                                                                                      ##STR705##                                                    ##STR706##                                                                                      ##STR707##                                                    ##STR708##                                                                                      ##STR709##                                                    ##STR710##                                                                                      ##STR711##                                                    ##STR712##                                                                                      ##STR713##                                                   ______________________________________                                         R.sup.g1                 Gn                                                    ______________________________________                                         Me                       Gc                                                    Et                       Gc                                                    Pr-n                     Gc                                                    Pr-iso                   Gc                                                    Bu-n                     Gc                                                    Bu-iso                   Gc                                                    Pen-n                    Gc                                                    CH.sub.2 Pr-cyc          Gc                                                    CH.sub.2 CH.sub.2 Py-cyc Gc                                                    CH.sub.2 CHCH.sub.2      Gc                                                    CH.sub.2 CHCHMe          Gc                                                    CH.sub.2 CCH             Gc                                                    CH.sub.2 CCMe            Gc                                                    CH.sub.2 CH.sub.2 OMe    Gc                                                    CH.sub.2 OMe             Gc                                                    CH.sub.2 CH.sub.2 SMe    Gc                                                    CH.sub.2 SMe             Gc                                                    CH.sub.2 SO.sub.2 Me     Gc                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Gc                                                    CH.sub.2 CF.sub.3        Gc                                                    CH.sub.2 CN              Gc                                                    CH.sub.2 CH.sub.2 CN     Gc                                                    CH.sub.2 NO.sub.2        Gc                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Gc                                                    CH.sub.2 COMe            Gc                                                    CH.sub.2 COEt            Gc                                                    CH.sub.2 COCHCH.sub.2    Gc                                                    CH.sub.2 CHCHCOMe        Gc                                                    CH.sub.2 CONMe.sub.2     Gc                                                    ______________________________________                                    

The compound of the present invention can be used as a herbicide for upland fields by any treating method such as soil treatment, soil admixing treatment or foliage treatment.

The dose of the compound of the present invention varies depending upon the application site, the season for application, the manner of application, the type of weeds to be controlled, the type of crop plants, etc. However, the dose is usually within a range of from 0.0001 to 10 kg, preferably from 0.005 to 5 kg, per hectare (ha), as the amount of the active ingredient.

Further, the compound of the present invention may be combined with other herbicides, various insecticides, fungicides, plant growth regulating agents, synergism agents and safeners at the time of the preparation of the formulations or at the time of the application, as the case requires.

Particularly, by the combined application with other herbicide, it can be expected to reduce the cost due to a decrease of the dose or to enlarge the herbicidal spectrum or obtain higher herbicidal effects due to a synergistic effect of the combined herbicides. In such a case, a plurality of known herbicides may be simultaneously combined. The herbicides of the type which can be used in combination with the compound of the present invention, may, for example, be compounds disclosed in Farm Chemicals Handbook (1990).

When the compound of the present invention is to be used as a herbicide, it is usually mixed with a suitable carrier, for instance, a solid carrier such as clay, talc, bentonite, diatomaceous earth or fine silica powder, or a liquid carrier such as water, an alcohol (such as isopropanol, butanol, benzyl alcohol or furfuryl alcohol), an aromatic hydrocarbon (such as toluene or xylene), an ether (such as anisole), a ketone (such as cyclohexanone or isophorone), an ester (such as butyl acetate), an acid amide (such as N-methylpyrrolidone), or a halogenated hydrocarbon (such as chlorobenzene). If desired, a surfactant, an emulsifier, a dispersing agent, a penetrating agent, a spreader, a thickener, an antifreezing agent, a coagulation preventing agent or a stabilizer may be added to prepare an optional formulation such as a liquid formulation, an emulsifiable concentrate, a wettable powder, a dry flowable, a flowable, a dust or a granule.

Cropland weeds to be controlled by the compound of the present invention include, for example, Solanaceae weeds such as Solanum nigrum and Datura stramonium, Malvaceae weeds such as Abutilon theophrasti and Side spinosa, Convolvulaceae weeds such as Ipomoea spps. e.g. Ipomoea purpurea, and Calystegia spps., Amaranthaceae weeds such as Amaranthus lividus and Amaranthus viridis, Compositae weeds such as Xanthium strumarium, Ambrosia artemisiaefolia, Helianthus annuu, Galinsoga ciliat, Cirsium arvense, Senecio vulgaris and Erigeron annus, Cruciferae weeds such as Rorippa indica, Sinapis arvensis and Capsella Bursapastris, Polygonaceae weeds such as Polygonum Blumei and Polygonum convolvulus, Portulacaceae weeds such as Portulaca oleracea, Chenopodiaceae weeds such as Chenopodium album, Chenopodium ficifolium and Kochia scoparis, Caryophyllaceae weeds such as Stellaria media, Scrophulariaceae weeds such as Veronica persica, Commelinaceae weeds such as Commelina communis, Labiatae weeds such as Lamium amplexicaule and Lamium purpureum, Euphorbiaceae weeds such as Euphorbia supina and Euphorbia maculata, Rubiaceae weeds such as Galium spurium, Galium aparine and Rubia akane, Violaceae weeds such as Viola arvensis, Leguminosae weeds such as Sesbania exaltata and Cassia obtusifolia, Graminaceous weeds such as Sorgham bicolor, Panicum dichotomiflorum, Sorghum halepense, Echinochloa crus-galli, Digitaria adscendens, Avena fatua, Eleusine indica, Setaria viridis and Alopecurus aegualis, and Cyperaceous weeds such as Cyperus rotundus and Cyperus esculentus.

Further, the compound of the present invention can be used as a paddy field herbicide by any treating method such as irrigated soil treatment or foliage treatment. Paddy weeds include, for example, Alismataceae weeds such as Alisma canaliculatum, Sagittaria trifolia and Sagittaria pygmaea, Cyperaceae weeds such as Cyperus difformis, Cyperus serotinus, Scirpus juncoides and Eleocharis kuroguwai, Scrothulariaceae weeds such as Lindemia pyxidaria, Potenderiaceae weeds such as Monochoria vaginalis, Potamogetonaceae weeds such as Potamogeton distinctus, Lythraceae weeds such as Rotala indica, and Gramineae weeds such as Echinochloa crus-galli.

The compound of the present invention can be applied to control various weeds not only in the agricultural and horticultural fields such as upland fields, paddy fields or orchards, but also in non-agricultural fields such as play grounds, non-used vacant fields or railway sides.

The compound of the present invention can easily be produced by selecting any one of the following reaction schemes 1 to 5. ##STR714## In the above formulas, Q, G and L are as defined above, and Z is a halogen atom.

Namely, the amine (2) is reacted with chlorosulfonyl isocyanate in a solvent such as tetrahydrofuran, dimethoxyethane, acetonitrile, propionitrile, dimethylformamide, dichloromethane, dichloroethane, benzene or toluene and then reacted with the imine (3) or (4) in the presence of a base such as triethylamine, pyridine, sodium hydride, sodium methoxide, sodium ethoxide, sodium hydroxide, potassium hydroxide or potassium carbonate, to obtain the compound of the present invention (1:X=O). ##STR715## In the above formulas, Q, G, L and Z are as defined above, and Y is a C₁₋₆ alkyl group or a phenyl group.

Namely, the reaction of the imine (3) or (4) with phenyl N-chlorosulfonyl carbamate (5:Y=phenyl group) or an alkyl N-chlorosulfonyl carbamate (5:Y=lower alkyl group), is conducted by using the carbamate derivative (5) in an amount of from 0.5 to 3.0 mols, per mol of the imine (3) or (4). Preferably, the amount is within a range of from 0.9 to 1.2 mols.

The reaction temperature may be selected optionally within a range of from -50° C. to 100° C., but it is preferably within a range of from -20° C. to 30° C.

This reaction can be carried out by using various bases. The amount of the base is from 0.5 to 4.0 mols per mol of the imine (3) or (4).

A suitable base may, for example, be an organic base such as triethylamine or pyridine, a metal hydride such as sodium hydride, an inorganic base such as sodium hydroxide, potassium hydroxide or potassium carbonate, or a metal alkoxide such as sodium methoxide or sodium ethoxide.

A suitable solvent for this reaction is a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as ethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzine or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethyl phosphorous triamide.

These solvents may be used alone or in combination as a mixture.

Particularly preferred is an ether or an amide.

Then, the phenyl N-substituted iminosulfonyl carbamate (6:X=O, Y=phenyl group) or the alkyl N-substituted substituted iminosulfonyl carbamate (6:X=O, Y=lower alkyl group) and the compound (2) are heated in a solvent such as benzene, toluene or dioxane to obtain the compound of the present invention (1:X=O). ##STR716## In the above formulas, Q, G, L and Y are as defined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted with the carbamate derivative (8) in a solvent such as acetone, acetonitrile or dioxane in the presence of an inorganic base such as potassium carbonate or an organic base such as triethylamine or 1,8-diazabicyclo 5.4.0!-7-undecene (DBU) to obtain the compound of the present invention (1:X=O). ##STR717## In the above formulas, Q, G, L, X and Y are as defined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted with chloroformic acid (thio)ester or carbonic acid (thio)ester in a solvent such as acetone, methyl ethyl ketone, acetonitrile, dioxane or tetrahydrofuran in the presence of a base such as potassium carbonate, triethylamine or pyridine to obtain the compound (6), which is then heated together with the compound (2) in a solvent such as toluene, benzene or dioxane to obtain the compound of the present invention (1). ##STR718## In the above formulas, Q and G are as defined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted with the isothiocyanate derivative (9) in a solvent such as acetone, acetonitrile, dioxane or tetrahydrofuran in the presence of an inorganic base such as potassium carbonate or an organic base such as triethylamine or DBU, to obtain the compound of the present invention (1:X=S, L=H).

The intermediates to be used in the present invention, i.e. the substituted iminosulfonamide derivative (7), the phenyl N-substituted iminosulfonyl(thio)carbamate (6:Y=phenyl group) and the alkyl N-substituted iminosulfonyl(thio)carbamate (6:Y=C₁₋₆ alkyl group) are also novel compounds.

The substituted iminosulfonamide derivative (7) can be synthesized from an imine (3) or (4) by the methods of the following Reaction Schemes 6 and 7. ##STR719## In the above formulas, Q and Z are as defined above.

In the Reaction Scheme 6, the reaction of tert-butanol with chlorosulfonyl isocyanate can be conducted by a method per se known, for example, in accordance with Japanese Unexamined Patent Publication No. 101323/1975.

The reaction of the imine (3) or (4) with tert-butylsulfamoyl chloride is carried out by using tert-butylsulfamoyl chloride in an amount of from 0.5 to 3.0 mols per mol of the imine (3) or (4). Preferably the amount is within a range of from 0.9 to 1.2 mols.

The reaction temperature may be selected optionally within a range of from -50° C. to 100° C. However, the temperature is preferably within a range of from -20° C. to 30° C.

This reaction can be conducted by using various bases. The amount of the base is from 0.5 to 4.0 mols per mol of the imine (3) or (4). Preferably, the amount is within a range of from 0.8 to 2.5 mols. A suitable base may, for example, be a metal hydride such as sodium hydride, an organic base such as triethylamine or pyridine, an inorganic base such as sodium hydroxide, potassium hydroxide or potassium carbonate, or a metal alkoxide such as sodium methoxide or sodium ethoxide.

A suitable solvent for the reaction is a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as ethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzine or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphorous triamide.

These solvents may be used alone or in combination as a mixture. Particularly preferred is an ether or an amide. ##STR720## In the above formulas, Q is as defined above.

In the Reaction Scheme 7, removal of the tert-butyl group is carried out by using trifluoroacetic acid.

The amount of trifluoroacetic acid may be selected optionally within a range of an equimolar amount to an excess amount. Trifluoroacetic acid may be used as a solvent without any particular problem.

The reaction temperature may be selected optionally within a range of from -50° C. to 80° C. The temperature is preferably within a range of from -20° C. to 30° C.

When a solvent is used for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as ethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzine or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphorous triamide, may be used. These solvents may be used alone or in combination as a mixture.

In Reaction Scheme 2, the phenyl N-chlorosulfonyl carbamate (5:Y=phenyl group) and the alkyl N-chlorosulfonyl carbamate (5:Y=lower alkyl group) can be synthesized by a method known per se, for example, in accordance with Chemische Berichte, vol. 96, p. 56 (1963).

The imines (3) and (4) to be used as the starting materials for the above reaction, can be synthesized, for example, in accordance with U.S. Pat. No. 4,237,302, Journal of Chemical Society, p. 307 (1956), Chemical and Pharmaceutical Bulletin, vol. 26, p. 3658 (1978), Journal of Organic Chemistry, vol. 30, p. 4298 (1965), East German Patent 291,757, Journal of American Chemical Society, vol. 93, p. 5552 (1971), U.S. Pat. No. 4,054,652, British Patent 752,003, Chemische Berichte, vol. 92, p. 1928 (1959), Journal of Medicinal Chemistry, vol. 6, p. 266 (1963), Chemical Abstracts, vol. 64, 14171e (1966), and Belgian Patent 654,416.

As representative examples, synthetic schemes for 2-imino-3-ethoxythiazolidine hydrobromide, 2-imino-3-n-propoxythiazolidine hydrobromide and 2-imino-3-methoxy-4,5-dimethylthiazoline hydrochloride will be shown as Reaction Schemes 8, 9 and 10. ##STR721##

THE BEST MODE FOR CARRYING OUT THE INVENTION

Now, syntheses of the compounds of the present invention will be described in detail as Reference Examples and working Examples. However, the present invention is by no means restricted to such specific Examples.

REFERENCE EXAMPLE a-1 Preparation of 2-imino-3-methylthiazol-4-ine hydroiodide ##STR722##

In 125 ml of dimethylformamide, 50 g (0.5 mol) of 2-aminothiazole was dissolved, and 90 g (0.63 mol) of methyl iodide was added thereto at room temperature. The mixture was further stirred at room temperature for 48 hours. Then, 1000 ml of ethyl acetate was added to the reaction mixture. Formed crystals were collected by filtration, washed with ethyl acetate and then dried to obtain 105 g of 2-imino-3-methylthiazol-4-ine hydroiodide.

Melting point: 181°-183° C.

The 2-imino-3-methylthiazol-4-ine hydroiodide was neutralized with potassium carbonate to obtain 2-imino-3-methylthiazol-4-ine.

Boiling point 55°-60° C./1 mmHg

REFERENCE EXAMPLE a-2 Preparation of 2-imino-3-n-butylthiazolidine ##STR723##

In 25 ml of dimethylformamide, 8.2 g (80 mmol) of 2-amino-2-thiazolidine was dissolved, and 18.4 g (100 mmol) of n-butyl iodide was added thereto at room temperature. The reaction mixture was heated and stirred at 60° C. for 10 hours and then left to cool to room temperature. The reaction mixture was added to 300 ml of ethyl acetate, and the mixture was stirred at room temperature for 10 minutes. A formed oily substance was separated by decantation from the ethyl acetate solution, and the same operation was repeated twice. Then, ethyl acetate contained in the oily substance was distilled off under reduced pressure to obtain 2-imino-3-n-butylthiazolidine hydroiodide as a crude product.

Then, the 2-imino-3-n-butylthiazolidine hydroiodide was stirred together with 5.28 g (80 mmol) of 85% potassium hydroxide in 300 ml of methanol at room temperature for one hour. Methanol was distilled off under reduced pressure. Then, 200 ml of chloroform was added to the residue, and precipitated insoluble matters were removed by filtration. Chloroform was distilled off under reduced pressure, and 6.9 g of 2-imino-3-n-butylthiazolidine was obtained by distillation under reduced pressure.

Boiling point: 85°-89° C./0.26 tort

REFERENCE EXAMPLE a-3 Preparation of 2-imino-1,3-dimethylimidazol-4-ine hydrochloride ##STR724##

16.9 g (150 mmol) of creatinine was dissolved in 100 ml of N, N-dimethylformamide. Then, 27.6 g (194 mmol) of methyl iodide was added thereto, and the mixture was heated to 50° C. and stirred at that temperature for 2 hours and further at room temperature overnight. To the reaction mixture, 500 ml of ethyl acetate was added, and crystals were collected by filtration. The obtained crystals were washed with ethyl acetate and dried to obtain 26.2 g of 2-imino-1,3-dimethylimidazolidin-4-one hydroiodide as white crystals.

Then, to 150 ml of a methanol solution containing 5.17 g (78.4 mmol) of 85% potassium hydroxide, 20 g (78.4 mmol) of 2-imino-1,3-dimethylimidazolidin-4-one hydroiodide was added, and the mixture was stirred at room temperature for 20 minutes. The solvent was distilled off under reduced pressure. Then, to the residue, 200 ml of chloroform was added, and insoluble matters were filtered off. The filtrate was dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure to obtain 9.0 g of 2-imino-1,3-dimethylimidazolidin-4-one.

800 mg (21.0 mmol) of lithium aluminum hydride was suspended in 20 ml of dry tetrahydrofuran, and 200 ml of a dry tetrahydrofuran solution containing 1.5 g (11.8 mmol) of 2-imino-1,3-dimethylimidazolidin-4-one, was added thereto at room temperature. The mixture was stirred at the same temperature overnight. Then, to the reaction mixture, 10 ml of ethyl acetate and then 5 ml of water were carefully added, and insoluble matters were filtered off. The filtrate was adjusted to pH 3 with concentrated hydrochloric acid, and then the solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethyl ether and ethanol to obtain 1.2 g of 2-imino-1,3-dimethylimidazol-4-ine hydrochloride.

Melting point: 168°-171° C.

The structures and the physical property values or characteristics of the compounds prepared by the same methods as the above Reference Examples a-1 to a-3 are presented in Tables 13a-1, 13a-2 and 13a-3.

                  TABLE 13a-1                                                      ______________________________________                                          ##STR725##                                                                                                    Physical property values                       R.sup.a1    R.sup.a2                                                                              R.sup.a3                                                                               HZ   or characteristics                             ______________________________________                                         C.sub.2 H.sub.5                                                                            H      H       HI   m.p. 113-114° C.                        C.sub.3 H.sub.7 -n                                                                         H      H       HI   m.p. 99-101° C.                         CH.sub.2 Ph H      H       HBr  m.p. 153-155° C.                        CH.sub.2 CO.sub.2 CH.sub.3                                                                 H      H       HBr  m.p. 174-177° C.                        CH.sub.2 CHCH.sub.2                                                                        H      H       HI   m.p. 113-116° C.                        CH.sub.2 CHCH                                                                              H      H       HBr  m.p. 148-153° C.                        CH.sub.2 CO.sub.2 C.sub.2 H.sub.5                                                          H      H       HBr  m.p. 166-167° C.                        CH(CH.sub.3)CO.sub.2 C.sub.2 H.sub.5                                                       H      H       HBr  m.p. 138-141° C.                        CH.sub.2 COCH.sub.3                                                                        H      H       HBr  m.p. 139-141° C.                        CH.sub.3    CH.sub.3                                                                              H       HI   m.p. 157-160° C.                        CH.sub.3    CH.sub.3                                                                              CH.sub.3                                                                               HI   m.p. 208-210° C.                        C.sub.3 H.sub.7 -n                                                                         CH.sub.3                                                                              H       HI   m.p. 166-168° C.                        C.sub.4 H.sub.9 -n                                                                         H      H       HI   m.p. 55-58° C.                          C.sub.5 H.sub.11 -n                                                                        H      H       --   b.p. 97-100° C./0.9 torr                CH.sub.2 CHCHCH.sub.3                                                                      H      H       HBr  m.p. 166-167° C.                        CH.sub.2 CHCHPh                                                                            H      H       HBr  m.p. 125-129° C.                        CH.sub.2 CH.sub.2 OCH.sub.3                                                                H      H       HBr  m.p. 141-142° C.                        C.sub.3 H.sub.7 -n                                                                         CH.sub.3                                                                              CH.sub.3                                                                               HI   m.p. 135-138° C.                        CH.sub.3    Ph     H       HI   m.p. 235-238° C.                        CH.sub.3    H      Cl      HI   m.p. 225-228° C.                        CH.sub.2 COPh                                                                              H      H       HBr  m.p. 207-208° C.                        CH.sub.2 OCH.sub.2 Ph                                                                      H      H       HCl  m.p. 99-104° C.                         CH.sub.3    H      Br      HI   m.p. 223-225° C.                        C.sub.3 H.sub.7 -n                                                                         H      Cl      HI   m.p. 182-184° C.                        CH(CH.sub.3).sub.2                                                                         H      H       --   b.p. 75-78° C./0.3 torr                 CH.sub.2 CN H      H       HBr  m.p. 154-155° C.                        CH.sub.2 CH(CH.sub.3).sub.2                                                                H      H       --   b.p. 78-81° C./0.3 torr                 C.sub.6 H.sub.13 -n                                                                        H      H       --   b.p. 110-112° C./                                                       0.45 torr                                      CH(CH.sub.3)C.sub.2 H.sub.5                                                                H      H       --   b.p. 83-90° C./0.4 torr                 CH.sub.2 OCH.sub.3                                                                         H      H       --   b.p. 80-81° C./0.5 torr                 CH.sub.2 C(Cl)CH.sub.2                                                                     H      H       HCl  m.p. 155-159° C.                        CH.sub.2 CHCHCl                                                                            H      H       HCl  m.p. 60-66° C.                          CH.sub.2 SCH.sub.3                                                                         H      H       --   b.p. 82-85° C./0.6 torr                 CH.sub.2 C(CH.sub.3)CH.sub.2                                                               H      H       HCl  m.p. 114-118° C.                        CH.sub.2 CHC(CH.sub.3).sub.2                                                               H      H       --   b.p. 90-102° C./0.3 torr                CH.sub.3    H      CH.sub.3                                                                               HI   m.p. 179-181° C.                        C.sub.3 H.sub.7 -n                                                                         H      CH.sub.3                                                                               HI   m.p. 152-154° C.                        CH.sub.3    H      OCH.sub.3                                                                              HI   m.p. 158-160° C.                        CH.sub.2 PhOMe-p                                                                           H      H       HCl  m.p. 163-165° C.                        CH.sub.2 PhCl-p                                                                            H      H       HCl  m.p. 157-159° C.                        CH.sub.2 C(Br)CH.sub.2                                                                     H      H       HBr  m.p. 165-168° C.                        CH.sub.2 CH.sub.2 Ph                                                                       H      H       HBr  m.p. 144-145° C.                        CH.sub.2 OC.sub.2 H.sub.5                                                                  H      H       HCl  m.p. 95-97° C.                          CH.sub.2 CCCH.sub.3                                                                        H      H       HBr  m.p. 167-169° C.                        ______________________________________                                    

                  TABLE 13a-2                                                      ______________________________________                                          ##STR726##                                                                                                    Physical property values                       R.sup.a1   R.sup.a4                                                                              R.sup.a5                                                                               HZ    or characteristics                             ______________________________________                                         CH.sub.3   H      H       HI    m.p. 147-150° C.                        C.sub.3 H.sub.7 -n                                                                        H      H       HI    m.p. 119-123° C.                        CH.sub.2 CHCH.sub.2                                                                       H      H       HI    m.p. 111-116° C.                        CH.sub.2 CCH                                                                              H      H       HBr   m.p. 118-122° C.                        C.sub.2 H.sub.5                                                                           H      H       --    b.p. 78-83° C./0.9 torr                 CH.sub.2 COCH.sub.3                                                                       H      H       HBr   m.p. 233-237° C.                        C.sub.5 H.sub.11 -n                                                                       H      H       --    b.p. 95-96° C./0.25 torr                CH.sub.2 CHCHCH.sub.3                                                                     H      H       --    b.p. 85-90° C./0.2 torr                 C.sub.6 H.sub.13 -n                                                                       H      H       --    b.p. 109-110° C./0.4 torr               CH.sub.3   H      CH.sub.3                                                                               --    Pale yellow oil                                C.sub.3 H.sub.7 -n                                                                        H      CH.sub.3                                                                               --    Pale yellow oil                                CH.sub.2 OCH.sub.3                                                                        H      H       HCl   White solid                                    CH.sub.2 C(Cl)CH.sub.2                                                                    H      H       HCl   m.p. 150-155° C.                        CH.sub.2 CHCHCl                                                                           H      H       HCl   m.p. 131-133° C.                        Ph         H      H       HCl   m.p. 224-226° C.                        ______________________________________                                    

                  TABLE 13a-3                                                      ______________________________________                                          ##STR727##                                                                                                     Physical property values                      R.sup.a1                                                                              R.sup.a2                                                                              R.sup.a3                                                                              R.sup.a6                                                                             HZ    or characteristics                            ______________________________________                                         C.sub.2 H.sub.5                                                                       H      H      CH.sub.3                                                                             HCl   Pale yellow solid                             C.sub.3 H.sub.7 -n                                                                    H      H      CH.sub.3                                                                             HCl   Pale yellow solid                             ______________________________________                                    

REFERENCE EXAMPLE b-1 Preparation of 2-imino-3-n-propylthiadiazol-4-ine hydroiodide ##STR728##

In 40 ml of dimethylformamide, 8.1 g (80 mmol) of 2-aminothiadiazole was dissolved, and 17.0 g (100 mmol) of n-propyl iodide was added thereto at room temperature.

The mixture was heated at 60° C. for 30 minutes and then left to cool, and then it was stirred at room temperature for 24 hours. Then, to the reaction mixture, 500 ml of ethyl acetate was added. Formed crystals were collected by filtration, washed with ethyl acetate and then dried to obtain 13.1 g of desired 2-imino-3-n-propylthiadiazol-4-ine hydroiodide.

Melting point: 121°-124° C.

The structures and the physical property values of the compounds prepared by the same method as in the above Reference Example b-1 are presented in Table 13b.

                  TABLE 13b                                                        ______________________________________                                          ##STR729##                                                                                                 Physical property values                          R.sup.b1     R.sup.b2                                                                               HZ      or characteristics                                ______________________________________                                         CH.sub.3     H       HI      m.p. 221-227° C.                           CH.sub.2 CHCH.sub.2                                                                         H       HBr     m.p. 131-132° C.                           CH.sub.2 CCH H       HBr     m.p. 114-117° C.                           CH.sub.2 COCH.sub.3                                                                         H       HBr     m.p. 198-200° C.                           CH.sub.3     CH.sub.3                                                                               HI      m.p. 117-121° C.                           ______________________________________                                    

REFERENCE EXAMPLE c-1 Preparation of 2-imino-3-n-propoxythiazolidine hydrobromide ##STR730##

22 g (197 mmol) of n-propoxyamine hydrochloride was dissolved in 100 ml of water, and 200 ml of ethylene dichloride was added thereto. Then, 27.2 g (197 mmol) of potassium carbonate was added in several times under cooling, and then 21.3 g (196 mmol) of ethyl chloroformate was dropwise added thereto at a temperature of not higher than 10° C. After raising the temperature to room temperature, the mixture was further stirred at the same temperature for 4 hours. The ethylene dichloride layer was separated, and then the aqueous layer was extracted twice with 100 ml of chloroform. The ethylene dichloride layer and the chloroform layer were put together, and washed with a saturated sodium chloride aqueous solution, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. 27 g of ethyl N-n-propoxycarbamate was obtained by distillation under reduced pressure.

Boiling point: 88° C./2.5 mmHg

8.73 g (218 mmol) of 60% sodium hydride was suspended in 200 ml of dry tetrahydrofuran, and 50 ml of a dry tetrahydrofuran solution containing 26.7 g (182 mmol) of ethyl N-n-propoxycarbamate, was dropwise added thereto under cooling with ice at a temperature of not higher than 10° C. After raising the temperature to room temperature, the mixture was stirred at the same temperature for 20 minutes and again cooled with ice. Then, 121.4 g (646 mmol) of 1,2-dibromoethane was added all at once. The temperature was gradually raised and then the mixture was refluxed under heating for 2 hours. the mixture was left to cool to room temperature, and the solvent was partially distilled off under reduced pressure. The residue was poured into 100 ml of ice water and extracted three times with 100 ml of chloroform. The chloroform layer was washed with a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and then 42.0 g of ethyl N-(2-bromoethyl)-N-n-propoxycarbamate was obtained by distillation under reduced pressure.

Boiling point: 97° C./0.4 mmHg

A mixture comprising 41.7 g (164 mmol) of ethyl N-(2-bromoethyl)-N-n-propoxycarbamate, 16.2 g (213 mmol) of thiourea and 200 ml of ethanol, was refluxed under heating for 5 hours. The mixture was left to cool, and then the solvent was distilled off under reduced pressure. Then, 300 ml of chloroform was added to the residue, and the mixture was stirred at room temperature for 10 minutes. After removing insoluble matters by filtration, chloroform was distilled off under reduced pressure. To the residue, ethyl ether and a small amount of water were added for crystallization. Then, the crystals were collected by filtration to obtain 50 g of S- 2-(N-ethoxycarbonyl-N-n-propoxy)aminoethyl!-isothiuronium hydrobromide.

Melting point: 74°-76° C.

5.0 g (15.2 mmol) of S- 2-(N-ethoxycarbonyl-N-n-propoxy)aminoethyl!isothiuronium hydrobromide and 0.27 g (15.0 mmol) of water were added to 30 ml of a 30% hydrogen bromide/acetic acid solution, and the mixture was heated and stirred at 55° C. for 4 hours. The mixture was left to cool, and acetic acid was distilled off under reduced pressure. To the residue, ethyl ether and a small amount of ethanol were added for crystallization. The crystals were collected by filtration to obtain 3.8 g of S- 2-(N-n-propoxy)aminoethyl!isothiuronium hydrobromide.

Melting point: 112°-113° C.

3.8 g (14.7 mmol) of S- 2-(N-n-propoxy)aminoethyl!-isothiuronium hydrobromide was added to 60 ml of ethanol, and the mixture was refluxed under heating for 3 hours. The mixture was left to cool, and then ethanol was distilled off under reduced pressure. To the residue, ethyl ether and a small amount of ethanol were added for crystallization. The crystals were collected by filtration to obtain 3.2 g of 2-imino-3-n-propoxythiazolidine hydrobromide.

Melting point: 117°-119° C.

REFERENCE EXAMPLE c-2 Preparation of 2-imino-3-methoxy-4-methylthiazol-4-ine hydrochloride ##STR731##

5.67 g (70 mmol) of sodium thiocyanate was dissolved in 12 ml of water, and the solution was heated to 80° C. 5.55 g (60 mmol) of chloroacetone was dropwise added thereto over a period of one hour, and the mixture was stirred at the same temperature for 3 hours. The mixture was cooled to room temperature, and then 60 ml of ethyl ether was added thereto. The aqueous layer was separated and removed. The ethyl ether layer was washed twice with 10 ml of water, and then the solvent was distilled off under reduced pressure to obtain 6.0 g of thiocyanoacetone.

2.30 g (20 mmol) of thiocyanoacetone and 1.67 g (20 mmol) of methoxyamine hydrochloride were dissolved in 10 ml of ethanol, and the solution was refluxed under heating for 5 hours. Ethanol was distilled off under reduced pressure. Then, to the obtained residue, 50 ml of ethyl acetate was added. Precipitated crystals were collected by filtration to obtain 3.34 g of 2-imino-3-methoxy-4-methylthiazol-4-ine hydrochloride.

Melting point: 145°-155° C. (decomposed)

The structures and the physical property values of the compounds prepared by the same methods as in Reference Examples c-1 and c-2 are presented in Tables 3c-1, 13c-2 and 13c-3.

                  TABLE 13c-1                                                      ______________________________________                                          ##STR732##                                                                                                    Physical property values                       R.sup.c1    R.sup.c2                                                                              R.sup.c3                                                                              HZ    or characteristics                             ______________________________________                                         C.sub.2 H.sub.5                                                                            H      H      HBr   m.p. 175-176° C.                        CH(CH.sub.3).sub.2                                                                         H      H      HBr   m.p. 150-152° C.                        CH.sub.3    H      H      HBr   Pale yellow glassy                             C.sub.4 H.sub.9 -n                                                                         H      H      HBr   m.p. 97-98° C.                          CH.sub.2 CCH                                                                               H      H      HBr   m.p. 139-140° C.                        CH.sub.2 CHCH.sub.2                                                                        H      H      HBr   m.p. 139-140° C.                        CH.sub.2 CHCHCl                                                                            H      H      HBr   m.p. 145-150° C.                        CH.sub.2 CH(CH.sub.3).sub.2                                                                H      H      HBr   m.p. 110-111° C.                        C.sub.5 H.sub.11 -n                                                                        H      H      HBr   Oil                                            CH.sub.2 C(Cl)CH.sub.2                                                                     H      H      HBr   m.p. 169-170° C.                        CH.sub.2 Ph H      H      HBr   m.p. 167-169° C.                        ______________________________________                                    

                  TABLE 13c-2                                                      ______________________________________                                          ##STR733##                                                                                                     Physical property values                      R.sup.c1                                                                               R.sup.c4                                                                              R.sup.c5                                                                              R.sup.c6                                                                            HZ    or characteristics                            ______________________________________                                         C.sub.2 H.sub.5                                                                        H      H      H    HBr   m.p. 209-210° C.                       ______________________________________                                    

                  TABLE 13c-3                                                      ______________________________________                                          ##STR734##                                                                    R.sup.c1                                                                             R.sup.c7                                                                              R.sup.c8                                                                              HZ   Physical property values or characteristics           ______________________________________                                         CH.sub.3                                                                             CH.sub.3                                                                              CH.sub.3                                                                              HCl  m.p. 150-155° C. (decomposed)                  ______________________________________                                    

REFERENCE EXAMPLE d-1 Preparation of 3-methyl-2-iminothiazolidin-4-one hydroiodide ##STR735##

11.6 g (0.1 mol) of pseudothiohydantoin was suspended in 150 ml of dimethylformamide, and 17 g (0.12 mol) of methyl iodide was added thereto. Then, the mixture was stirred at 60° C. for one hour. After being left to cool, the reaction mixture was poured into 1000 ml of ethyl acetate, and precipitated crystals were collected by filtration to obtain 15 g of 3-methyl-2-iminothiazolidin-4-one hydroiodide as pale yellow crystals.

Melting point: 237°-238° C.

REFERENCE EXAMPLE d-2 Preparation of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide ##STR736##

9.04 g (80 mmol) of creatinine was suspended in 50 ml of dimethylformamide, and 17.0 g (100 mmol) of n-propyl iodide was added thereto. Then, the mixture was heated and stirred within a range of from 70° C. to 80° C. until creatinine was completely dissolved. The mixture was left to cool, and 500 ml of ethyl acetate was added thereto. Precipitated crystals were collected by filtration to obtain 10.6 g of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide.

Melting point: 159°-161° C.

The 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide was neutralized in accordance with the following method to obtain 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one.

2.83 g (10 mmol) of the 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide was added to 25 ml of methanol containing 0.66 g (10 mmol) of 85% potassium hydroxide, and the mixture was stirred at room temperature for one hour. Methanol was distilled off under reduced pressure, and chloroform was added to the residue. Precipitated crystals were removed by filtration. Chloroform was distilled off under reduced pressure to obtain 1.16 g of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one as an oily substance.

The structures and the physical property values of the compounds prepared by the same methods as in Reference Examples d-1 and d-2, are presented in Table 13d.

                  TABLE 13d                                                        ______________________________________                                          ##STR737##                                                                                                    Physical property values                       R.sup.d1   R.sup.d4                                                                              R.sup.d5                                                                               HZ    or characteristics                             ______________________________________                                         CH.sub.3   H      CH.sub.3                                                                               HI    m.p. 215-216° C.                        C.sub.2 H.sub.5                                                                           H      CH.sub.3                                                                               HI    m.p. 220-222° C.                        CH.sub.2 CHCH.sub.2                                                                       H      CH.sub.3                                                                               HBr   m.p. 117-119° C.                        CH.sub.2 CCH                                                                              H      CH.sub.3                                                                               HBr   m.p. 228-230° C.                        CH.sub.2 COCH.sub.3                                                                       H      CH.sub.3                                                                               HBr   m.p. 188-190° C.                        CH.sub.2 CO.sub.2 CH.sub.3                                                                H      CH.sub.3                                                                               HBr   m.p. 201-203° C.                        CH.sub.2 OCH.sub.3                                                                        H      CH.sub.3                                                                               HCl   m.p. 198-199° C.                        CH.sub.2 SCH.sub.3                                                                        H      CH.sub.3                                                                               HCl   m.p. 200-210° C.                                                        (decomposed)                                   ______________________________________                                    

REFERENCE EXAMPLE e-1 Preparation of 3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine ##STR738##

1.3 g (11.4 mmol) of 2-amino-6H-1,3-thiazine was dissolved in 4 ml of dimethylformamide, and 2.4 g (14.1 mmol) of n-propyl iodide was added thereto. The mixture was heated at 50° C. for one hour and then stirred at room temperature overnight. To the reaction solution, 100 ml of ethyl acetate was added, and the mixture was stirred and then left to stand still. Then, the ethyl acetate layer was separated and removed by decantation. Then, the residual oily substance was dissolved in 50 ml of methanol, and 30 ml of a methanol solution containing 0.75 g (11.4 mmol) of 85% potassium hydroxide, was added thereto at room temperature. The mixture was further stirred at the same temperature for one hour, and then methanol was distilled off under reduced pressure. To the residue, 60 ml of chloroform was added, and insoluble matters were removed by filtration. Then, the filtrate was concentrated under reduced pressure. The residual oily substance was purified by alumina column chromatography (eluent: chloroform) to obtain 0.4 g of 3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine as an oily substance.

REFERENCE EXAMPLE 2-e Preparation of 3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine ##STR739##

3.13 g (27 mmol) of 2-amino-4,5-dihydro-6H-1,3-thiazine was dissolved in 20 ml of isopropyl alcohol, and 4.26 g (30 mmol) of methyl iodide was added thereto. The mixture was refluxed under heating for one hour, and then left to cool. The solvent was distilled off under reduced pressure. Then, the residual oily substance was dissolved in 200 ml of methanol, and a 70 ml of a methanol solution containing 1.68 g (25.5 mmol) of 85% potassium hydroxide, was added thereto at room temperature. The mixture was stirred at the same temperature for 5 minutes, and then methanol was distilled off under reduced pressure. To the residue, 300 ml of chloroform was added and then dried over anhydrous sodium sulfate. Inorganic substances were removed by filtration, and then chloroform was distilled off under reduced pressure to obtain 3 g of 3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine as a pale red oily substance.

The structures and the characteristics of the compounds prepared by the same methods as in Reference Examples e-1 and e-2, are presented in Tables 13e-1 and 13e-2.

                  TABLE 13e-1                                                      ______________________________________                                          ##STR740##                                                                                                  Physical property values                         R.sup.e1  R.sup.e2                                                                              R.sup.e3                                                                               R.sup.e4                                                                            or characteristics                               ______________________________________                                         CH.sub.3  H      H       H    Oil                                              CH.sub.2 OCH.sub.3                                                                       H      H       H    Oil                                              ______________________________________                                    

                  TABLE 13e-2                                                      ______________________________________                                          ##STR741##                                                                                                  Physical property values                         R.sup.e1  R.sup.e8                                                                              R.sup.e9                                                                              R.sup.e10                                                                            or characteristics                               ______________________________________                                         C.sub.3 H.sub.7 -n                                                                       H      H      H     Oil                                              ______________________________________                                    

REFERENCE EXAMPLE f-1 Preparation of 2-imino-3-methyloxazolidine hydroiodide ##STR742##

15 g (122 mmol) of 2-amino-2-oxazoline hydrochloride was stirred with 8.4 g (128 mmol) of 85% potassium hydroxide in 400 ml of methanol at room temperature for one hour. Methanol was distilled off under reduced pressure, and then 500 ml of chloroform was added. Precipitated insoluble substances were removed by filtration. Chloroform was distilled off under reduced pressure to obtain 10.5 g of 2-amino-2-oxazoline.

Then, 10.5 g of 2-amino-2-oxazoline was dissolved in 40 ml of dimethylformamide, and 22 g (155 mmol) of methyl iodide was added thereto at room temperature. The mixture was further stirred at room temperature for 48 hours. Then, 1000 ml of ethyl acetate was added to the reaction mixture. Formed crystals were collected by filtration, washed with ethyl acetate and then dried to obtain 23 g of 2-imino-3-methyloxazolidine hydroiodide.

Melting point: 165°-169° C.

The structures and characteristics of the compounds prepared by the same method as in Reference Example f-1 are presented in Table 13f.

                  TABLE 13f                                                        ______________________________________                                          ##STR743##                                                                                                   Physical property values                        R.sup.f1   R.sup.f5                                                                              R.sup.f6                                                                              HZ    or characteristics                              ______________________________________                                         CH.sub.2 CHCH.sub.2                                                                       H      H      HBr   Glassy                                          ______________________________________                                    

REFERENCE EXAMPLE g-1 Preparation of N,N-dimethyl-S-methylisothiourea hydroiodide ##STR744##

35 g (0.5 mol) of N,N-dimethylcyanamide was dissolved in a mixed solution of 70 ml of pyridine and 70 ml of triethylamine, and the solution was heated to 60° C. Hydrogen sulfide gas was introduced thereinto for 30 minutes. Then, the reaction mixture was left to cool to room temperature, and 300 ml of ethyl ether was added thereto. Precipitated crystals were collected by filtration and then washed with ethyl ether to obtain 48 g of N,N-dimethylthiourea as pale brown crystals.

Melting point: 163°-164° C.

10.4 g (0.1 mol) of N,N-dimethylthiourea was suspended in 80 ml of ethanol, and 17 g (0.12 mol) of methyl iodide was added thereto. The mixture was refluxed under heating for 30 minutes. The reaction mixture was left to cool to room temperature, and then the solvent was distilled off under reduced pressure. The obtained crystals were washed with ethyl ether, collected by filtration and dried to obtain 20 g of N,N-dimethyl-S-methylisothiourea hydroiodide as yellow crystals.

Melting point: 84°-85° C.

REFERENCE EXAMPLE g-2 Preparation of N-ethyl-N-methyl-S-methylisothiourea hydroiodide ##STR745##

7.08 g (120 mmol) of N-ethyl-N-methylamine was dissolved in 80 ml of dry acetone, and the solution was cooled to 0° C. 13.1 g (100 mmol) of ethoxycarbonyl isothiocyanate was dropwise added thereto. Then, the reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 2 hours. The solvent was distilled off under reduced pressure. To the obtained residue, 80 ml of concentrated hydrochloric acid was added. The reaction temperature was raised to 80° C., and the mixture was further stirred at the same temperature for 5 hours. Then, it was cooled to 0° C., and then ammonium carbonate was gradually added to neutralize the reaction mixture (pH=6 to 7). After adding a small amount of water, the mixture was extracted three times with 100 ml of ethyl acetate. The ethyl acetate layer was washed with water and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethanol/n-hexane to obtain 5.8 g of N-ethyl-N-methylthiourea as white crystals. Melting point: 124°-125° C.

5.8 g (49 mmol) of N-ethyl-N-methylthiourea was dissolved in 10 ml of N,N-dimethylformamide. 8.8 g (62 mmol) of methyl iodide was added at room temperature, and the mixture was stirred at room temperature for 15 hours. 500 ml of ethyl acetate was added to the mixture, and precipitated crystals were collected by filtration and then washed with ethyl acetate to obtain 3.1 g of N-ethyl-N-methyl-S-methylisothiourea hydroiodide as pale yellow crystals.

Melting point: 94°-97° C.

REFERENCE EXAMPLE g-3 Preparation of N-methoxy-N-methyl-S-methylisothiourea hydroiodide ##STR746##

1.83 g (30 mmol) of N-methoxy-N-methylamine was dissolved in 20 ml of dichloromethane, and the solution was cooled to 0° C. 3.93 g (30 mmol) of ethoxycarbonyl isothiocyanate was dropwise added thereto. Then, the reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 15 hours. The solvent was distilled off under reduced pressure, and to the obtained residue, 20 ml of concentrated hydrochloric acid was added. The reaction temperature was raised to 80° C., and the mixture was further stirred at the same temperature for 5 hours. Then, the mixture was cooled to 0° C., and then ammonium carbonate was gradually added to neutralize the reaction mixture (pH=6 to 7). After adding 10 ml of water, the mixture was extracted three times with 50 ml of ethyl acetate. The ethyl acetate layer was washed with water and then dried over anhydrous magnesium sulfate. Then, the solvent was distilled off under reduced pressure to obtain 2.0 g of N-methoxy-N-methylthiourea as pale yellow crystals. Melting point: 30°-32° C

1.76 g (14.7 mmol) of N-methoxy-N-methylthiourea was dissolved in 5 ml of N,N-dimethylformamide. 2.09 g (14.7 mmol) of methyl iodide was added thereto at room temperature, and the mixture was stirred at room temperature for 15 hours. 500 ml of ethyl acetate was added thereto, and precipitated crystals were collected by filtration and then washed with ethyl acetate to obtain 2.7 g of N-methoxy-N-methyl-S-methylisothiourea hydroiodide as pale yellow crystals.

Melting point: 122°-124° C.

The structures and physical property values or characteristics of the compounds prepared by the same methods as in Reference Examples g-1 to g-3 are presented in Table 13g.

                  TABLE 13g                                                        ______________________________________                                          ##STR747##                                                                                                      Physical                                                                       property values                              R.sup.g1   R.sup.g2   R.sup.g3                                                                              HZ   or characteristics                           ______________________________________                                         C.sub.2 H.sub.5                                                                           CH.sub.3   CH.sub.3                                                                              HI   m.p. 93-94° C.                        C.sub.3 H.sub.7 -n                                                                        CH.sub.3   CH.sub.3                                                                              HI   m.p. 54-55° C.                        CH.sub.2 CHCH.sub.2                                                                       CH.sub.3   CH.sub.3                                                                              HBr  m.p. 148-149° C.                      CH.sub.2 CCH                                                                              CH.sub.3   CH.sub.3                                                                              HBr  m.p. 113-114° C.                      CH.sub.3   CH.sub.3 CO                                                                               CH.sub.3                                                                              --   Glassy                                       CH.sub.3   (CH.sub.2).sub.4                                                                             HI     m.p. 121-123° C.                        CH.sub.3   C.sub.3 H.sub.7 -n                                                                        CH.sub.3                                                                              HI   m.p. 126-127° C.                      CH.sub.3   Ph         CH.sub.3                                                                              HI   m.p. 170-173° C.                      CH.sub.3   C.sub.2 H.sub.5 O                                                                         CH.sub.3                                                                              HI   m.p. 114-115° C.                      CH.sub.3   n-C.sub.3 H.sub.7 O                                                                       CH.sub.3                                                                              HI   m.p. 75-76° C.                        CH.sub.3   CH.sub.2 CHCH.sub.2                                                                       CH.sub.3                                                                              HI   m.p. 116-118° C.                      ______________________________________                                    

EXAMPLE a-1 Preparation of 1-(3-methyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR748##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto within a range of from -10° C. to -5° C. The reaction temperature was raised to 0° C., and the mixture was stirred for 5 minutes. The reaction mixture was again cooled to -30° C., and 1.14 g (10 mmol) of 2-imino-3-methylthiazol-4-ine and 1.11 g (11 mmol) of triethylamine dissolved in 10 ml of dry tetrahydrofuran were dropwise added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure. Then, water was added to the obtained residue. Precipitated crystals were collected by filtration and washed with acetonitrile to obtain 1.5 g of desired 1-(3-methyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 214°-215° C.

EXAMPLE a-2 Preparation of 1-(3-n-propyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR749##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at a temperature of not higher than -20° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to a temperature of not higher than -20° C. Then, 2.70 g (10 mmol) of 2-imino-3-n-propylthiazol-4-ine hydroiOdide and 2.22 g (22 mmol) of triethylamine dissolved in 30 ml of dry tetrahydrofuran were dropwise added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure. Then, water was added to the residue, and the mixture was extracted three times with chloroform. The chloroform layer was washed Sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. The obtained crystals were washed with ethyl ether to obtain 3 g of desired 1-(3-n-propyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 166°-167° C.

EXAMPLE a-3 Preparation of 1-(3-n-butylthiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR750##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -40° C. The reaction temperature was raised to 0° C., and then the reaction mixture was cooled again to -60° C. Then, 1.90 g (12 mmol) of 2-imino-3-n-butylthiazolidine suspended in 40 ml of dry tetrahydrofuran containing 1.33 g (13 mmol) of triethylamine, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure. Then, water was added to the residue, and the mixture was extracted three times with chloroform. The chloroform layer was washed sequentially with water and a saturated sodium chloride aqueous solution, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. The obtained crystals were washed with ethyl ether to obtain 2.8 g of desired 1-(3-n-butylthiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 139°-140° C.

EXAMPLE a-4 Preparation of 1-(1,3-dimethyl-4-imidazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR751##

540 mg (3.46 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 490 mg (3.46 mmol) of chlorosulfonyl isocyanate was dropwise added in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to -20° C. Then, a mixture comprising 600 mg (4.07 mmol) of 2-imino-1,3-dimethylimidazol-4-ine hydrochloride, 820 mg (8.13 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 3 hours. Then, the solvent was distilled off under reduced pressure. Then, 60 ml of water was added to the obtained residue, and crystals were collected by filtration. The obtained crystals were washed with a solvent mixture of ethyl ether, acetonitrile and acetone to obtain 200 mg of desired 1-(1,3-dimethyl-4-imidazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 201°-203° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples a-1 to a-4 are presented in Tables 14a-1, 14a-2 and 14a-3.

                                      TABLE 14a-1                                  __________________________________________________________________________      ##STR752##                                                                    Compound                            m.p.                                       No.   R.sup.a1 R.sup.a2                                                                          R.sup.a3                                                                           L  A B    D   (°C.)                               __________________________________________________________________________     4-a   CH.sub.2 CO.sub.2 CH.sub.3                                                              H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          166-167                                    5-a   CH.sub.2 Ph                                                                             H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          177-178                                    6-a   C.sub.2 H.sub.5                                                                         H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          189-190                                    7-a   CH.sub.2 CHCH.sub.2                                                                     H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          165-166                                    8-a   CH.sub.2 C CH                                                                           H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          183-184                                    9-a   CH.sub.2 CO.sub.2 C.sub.2 H.sub.5                                                       H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          137-138                                    10-a  CH.sub.2 COCH.sub.3                                                                     H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          180-181                                    11-a  CH(CH.sub.3)CO.sub.2 C.sub.2 H.sub.5                                                    H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          131-132                                    12-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           CH.sub.3                                                                           167-170                                    13-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH                                                                               CH.sub.3                                                                            CH.sub.3                                                                           155-158                                    14-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH                                                                               OCHF.sub.2                                                                          OCHF.sub.2                                                                         152-154                                    15-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH                                                                               OCHF.sub.2                                                                          CH.sub.3                                                                           143-145                                    16-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OCH.sub.3                                                                           CH.sub.3                                                                           174-176                                    17-a  CH.sub.3 CH.sub.3                                                                          H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          211-213                                    18-a  CH.sub.3 CH.sub.3                                                                          CH.sub.3                                                                           H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          203-205                                    19-a  C.sub.3 H.sub.7 -n                                                                      CH.sub.3                                                                          H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          176-178                                    20-a  C.sub.4 H.sub.9 -n                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          149-151                                    21-a  C.sub.5 H.sub.11 -n                                                                     H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          160-161                                    22-a  CH.sub.2 CHCHCH.sub.3                                                                   H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          123-125                                    23-a  CH.sub.2 CHCHPh                                                                         H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          180-181                                    27-a  CH.sub.2 CH.sub.2 OCH.sub.3                                                             H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          137.5-138.5                                28-a  C.sub.3 H.sub.7 -n                                                                      CH.sub.3                                                                          CH.sub.3                                                                           H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          199-201                                    29-a  CH.sub.3 Ph H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          196-198                                    30-a  CH.sub.3 H  Cl  H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          198-201                                    31-a  CH.sub.3 H  Br  H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          209-211                                    32-a  C.sub.3 H.sub.7 -n                                                                      H  Cl  H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          139-142                                    33-a  CH.sub.2 OCH.sub.2 Ph                                                                   H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          168-169                                    35-a  C.sub.6 H.sub.13 -n                                                                     H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          173-175                                    36-a  CH.sub.2 CH(CH.sub.3).sub.2                                                             H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          177-179                                    37-a  CH(CH.sub.3).sub.2                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          175.5-176.5                                38-a  CH.sub.2 OCH.sub.3                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          173-174                                    39-a  CH(CH.sub.3)C.sub.2 H.sub.5                                                             H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          81-82                                      43-a  CH.sub.2 SCH.sub.3                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          181-183                                    44-a  CH.sub.2 CN                                                                             H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          183-183.5                                  45-a  CH.sub.2 C(Cl)CH.sub.2                                                                  H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          174-175                                    46-a  C.sub.3 H.sub.7 -n                                                                      H  H   CH.sub.3                                                                          CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          172-173                                    47-a  C.sub.4 H.sub.9 -n                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          147-149                                    48-a  CH.sub.2 CHCHCl                                                                         H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          165-167                                    49-a  CH.sub.2 C(CH.sub.3)CH.sub.2                                                            H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          177-179                                    52-a  CH.sub.3 H  CH.sub.3                                                                           H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          206-208                                    53-a  C.sub.3 H.sub.7 -n                                                                      H  CH.sub.3                                                                           H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          152-154                                    54-a  CH.sub.3 H  OCH.sub.3                                                                          H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          187-190                                    55-a  CH.sub.2 CHC(CH.sub.3).sub.2                                                            H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          170-171                                    57-a  CH.sub.2 CH.sub.2 Ph                                                                    H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          182-184                                    58-a  CH.sub.2 PhOMe-p                                                                        H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          109-110                                    60-a  CH.sub.2 PhCl-p                                                                         H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          182-183                                    61-a  CH.sub.2 C(Br)CH.sub.2                                                                  H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          167-168                                    63-a  CH.sub.2 OC.sub.2 H.sub.5                                                               H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          177-178                                    65-a  CH.sub.2 C CCH.sub.3                                                                    H  H   H  CH                                                                               OCH.sub.3                                                                           OCH.sub.3                                                                          184-186                                    68-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           Cl  165-168                                    72-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH                                                                               OCH.sub.3                                                                           OCHF.sub.2                                                                         193-195                                    73-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OCH.sub.3                                                                           OCH.sub.3                                                                          156-158                                    79-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OC.sub.2 H.sub.5                                                                    CH.sub.3                                                                           151-153                                    80-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OCH.sub.3                                                                           C.sub.2 H.sub.5                                                                    141-143                                    82-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OCH.sub.3                                                                           CH.sub.2 Cl                                                                        144-146                                    83-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH                                                                               CF.sub.3                                                                            Cl  146-148                                    84-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OCH.sub.3                                                                           C.sub.3 H.sub.7 -n                                                                 159-160                                    85-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OCH.sub.3                                                                           CF.sub.3                                                                           149-150                                    86-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N OC.sub.3 H.sub.7 -n                                                                 CH.sub.3                                                                           176-178                                    __________________________________________________________________________

                                      TABLE 14a-2                                  __________________________________________________________________________      ##STR753##                                                                    Compound                        m.p.                                           No.   R.sup.a1 R.sup.a4                                                                          R.sup.a5                                                                          A  B   D   (°C.)                                   __________________________________________________________________________      3-a  CH.sub.3 H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          204-206                                        24-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          172-173                                        25-a  CH.sub.2 CHCH.sub.2                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          177-178                                        26-a  CH.sub.2 CCH                                                                            H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          188-190                                        34-a  C.sub.2 H.sub.5                                                                         H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          170-172                                        41-a  CH.sub.2 CHCHCH.sub.3                                                                   H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          133-134                                        42-a  C.sub.5 H.sub.11 -n                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          132-134                                        50-a  CH.sub.2 COCH.sub.3                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          186-188                                        51-a  C.sub.6 H.sub.13 -n                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          163-165                                        56-a  CH.sub.3 H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          190-191                                        59-a  CH.sub.2 CHCHCl                                                                         H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          155-156                                        62-a  CH.sub.2 C(Cl)CH.sub.2                                                                  H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          190-192                                        64-a  CH.sub.2 OCH.sub.3                                                                      H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          169-170                                        70-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          Cl  144-146                                        71-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          OCHF.sub.2                                                                         144-145                                        74-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           175-177                                        75-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH CH.sub.3                                                                           CH.sub.3                                                                           166-168                                        76-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCHF.sub.2                                                                         OCHF.sub.2                                                                         173-174                                        77-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH CH.sub.3                                                                           Cl  155-158                                        78-a  C.sub.3 H.sub.7 -n                                                                      H  H  N  OCH.sub.3                                                                          CH.sub.3                                                                           184-186                                        81-a  Ph       H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          178-180                                        __________________________________________________________________________

                  TABLE 14-a3                                                      ______________________________________                                          ##STR754##                                                                    Com-                                                                           pound                                         m.p.                             No.    R.sup.a1                                                                               R.sup.a2                                                                             R.sup.a3                                                                           R.sup.a6                                                                            A   B     D     (°C.)                     ______________________________________                                         67-a   C.sub.2 H.sub.5                                                                        H     H   CH.sub.3                                                                            CH  OCH.sub.3                                                                            OCH.sub.3                                                                            178-180                          69-a   C.sub.3 H.sub.7 -n                                                                     H     H   CH.sub.3                                                                            CH  OCH.sub.3                                                                            OCH.sub.3                                                                            167-169                          ______________________________________                                    

EXAMPLE b-1 Preparation of 1-(3-n-propyl-thiadiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR755##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added at -40° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to -40° C. Then, 2.58 g (9.5 mmol) of 2-imino-3-n-propylthiadiazol-4-ine hydroiodide suspended in 40 ml of dry tetrahydrofuran containing 2.22 g (22 mmol) of triethylamine, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The mixture was extracted three times with chloroform. The chloroform layer was washed sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile to obtain 2.25 g of desired 1-(3-n-propyl-4-thiadiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 189°-190° C.

The structures and the physical property values of the compounds prepared by the same method as in Example b-1 are presented in Table 14b.

                  TABLE 14b                                                        ______________________________________                                          ##STR756##                                                                    Com-                                                                           pound                                    m.p.                                  No.    R.sup.b1   R.sup.b2                                                                              A   B     D     (°C.)                          ______________________________________                                         2-b    CH.sub.3   H      CH  OCH.sub.3                                                                            OCH.sub.3                                                                            216-217                               3-b    CH.sub.2 CHCH.sub.2                                                                       H      CH  OCH.sub.3                                                                            OCH.sub.3                                                                            197-198                               4-b    CH.sub.2 CCH                                                                              H      CH  OCH.sub.3                                                                            OCH.sub.3                                                                            196-198                               5-b    CH.sub.2 COCH.sub.3                                                                       H      CH  OCH.sub.3                                                                            OCH.sub.3                                                                            206-208                               6-b    CH.sub.3   CH.sub.3                                                                              CH  OCH.sub.3                                                                            OCH.sub.3                                                                            203.5-204.5                           ______________________________________                                    

EXAMPLE c-1 Preparation of 1-(3-ethoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR757##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of -10° C. to -5° C. The reaction temperature was raised to 0° C., and the mixture was stirred for 5 minutes. The reaction mixture was cooled again to -30° C., and 2.72 g (12 mmol) of 2-imino-3-ethoxythiazolidine hydrobromide and 2.43 g (24 mmol) of triethylamine suspended in 10 ml of dry tetrahydrofuran were gradually added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 20 minutes. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. Precipitated crystals were extracted three times with 100 ml of chloroform, and the extract was washed once with 100 ml of water and dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with ethyl ether and acetonitrile to obtain 2.1 g of desired 1-(3-ethoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyridimin-2-yl)urea.

Melting point: 175°-176° C.

EXAMPLE c-2 Preparation of 1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR758##

0.62 g (4.0 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 0.57 g (4.0 mmol) of chlorosulfonyl isocyanate was dropwise added at -50° C. The reaction temperature was raised to room temperature, and then the reaction mixture was cooled again to -50° C. Then, 1.2 g (5.0 mmol) of 2-imino-3-n-propoxythiazolidine hydrobromide suspended in 20 ml of dry tetrahydrofuran containing 1.01 g (10.0 mmol) of triethylamine, was added thereto. The reaction temperature was gradually raised to room temperature, and the mixture was further stirred at the same temperature for 10 minutes. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The mixture was extracted three times with 50 ml of chloroform. The chloroform layer was washed with a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. To the obtained residue, ethyl ether and a small amount of acetonitrile were added for crystallization. The crystals were collected by filtration to obtain 0.65 g of desired 1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyridimin-2-yl)urea.

Melting point: 173°-175° C.

EXAMPLE c-3 Preparation of 1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxytriazin-2-yl)urea ##STR759##

3.76 g (40.0 mmol) of phenol was dissolved in 40 ml of dry tetrahydrofuran, and 5.66 g (40.0 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -50° C. The reaction temperature was raised to room temperature, and then the reaction mixture was cooled again to -50° C. Then, 10.6 g (44 mmol) of 2-imino-3-n-propoxythiazolidine hydrobromide suspended in 20 ml of dry acetonitrile containing 8.08 g (80 mmol) of triethylamine, was added thereto. The reaction temperature was gradually raised to room temperature, and the mixture was further stirred at the same temperature for 10 minutes. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The mixture was extracted three times with 70 ml of chloroform. The chloroform layer was washed with a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. To the obtained residue, ethyl ether and a small amount of acetonitrile were added for crystallization. Then, the crystals were collected by filtration to obtain 14 g of phenyl N-(3-n-propoxythiazolidine-2-sulfonylimino)carbamate. Then, 0.72 g (2.0 mmol) of the obtained carbamate was dissolved in 30 ml of dry dioxane, and 0.23 g (1.5 mmol) of 2-amino-4,6-dimethoxytriazine was added thereto. The mixture was refluxed under heating for 4 hours. The solvent was distilled off under reduced pressure, and ethyl ether and a small amount of acetonitrile were added for crystallization. Then, the crystals were collected by filtration to obtain 0.3 g of desired 1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxytriazin-2-yl)urea.

Melting point: 166°-167° C.

EXAMPLE c-4 Preparation of 1- 3-(3-chloroallyloxy)thiazolidine-2-sulfonylimino!-3-(4-methyl-6-methoxytriazin-2-yl)urea ##STR760##

0.84 g (6 mmol) of 2-amino-4-methyl-6-methoxytriazine was suspended in 20 ml of dry tetrahydrofuran, and 0.85 g (6 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at room temperature. A heat was generated mildly, and the reaction mixture turned to a pale yellow solution. Then, 1.64 g (6 mmol) of 2-imino-3-(3-chloroallyloxy)thiazolidine hydrobromide and 1.43 g (14 mmol) of triethylamine suspended in 15 ml of dry tetrahydrofuran were gradually added thereto, and the mixture was further stirred at room temperature for 30 minutes. The solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The resulting oily substance was extracted three times with 80 ml of chloroform. The extract solution was washed once with 100 ml of water and dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with ethyl ether and acetonitrile to obtain 1.2 g of desired 1- 3-(3-chloroallyloxy)thiazolidine-2-sulfonylimino!-3-(4-methyl-6-methoxytriazin-2-yl)urea.

Melting point: 145°-147° C.

EXAMPLE c-5 Preparation of 1-(3-methoxy-4-methyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR761##

0.78 g (5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 10 ml of dry tetrahydrofuran, and 0.71 g (5 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was stirred for 5 minutes. The mixture was cooled again to -20° C., and 0.90 g (5 mmol) of 2-imino-3-methoxy-4-methylthiazol-4-ine hydrochloride and 1.11 g (11 mmol) of triethylamine suspended in 10 ml of dry tetrahydrofuran, was gradually added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 20 minutes. The solvent was distilled off under reduced pressure, and then water was added to the obtained residue. Precipitated crystals were extracted three times with 50 ml of chloroform. The extract solution was washed once with 50 ml of water and dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with ethyl ether and acetonitrile to obtain 1.02 g of desired 1-(3-methoxy-4-methyl-4-thiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 183°-185° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples c-1 to c-5 are presented in Tables 14c-1, 14c-2 and 14c-3.

                                      TABLE 14c-1                                  __________________________________________________________________________      ##STR762##                                                                    Compound No.                                                                          R.sup.c1                                                                               R.sup.c2                                                                          R.sup.c3                                                                         A  B    D   m.p. (°C.)                              __________________________________________________________________________     2-c    C.sub.2 H.sub.5                                                                        H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           182-183                                        3-c    C.sub.2 H.sub.5                                                                        H  H N  OCH.sub.3                                                                           CH.sub.3                                                                           155-156                                        4-c    C.sub.2 H.sub.5                                                                        H  H CH CH.sub.3                                                                            CH.sub.3                                                                           152-153                                        5-c    CH(CH.sub.3).sub.2                                                                     H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          175-178                                        6-c    CH.sub.3                                                                               H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          193-194                                        7-c    CH.sub.3                                                                               H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           183-185                                        11-c   CH(CH.sub.3).sub.2                                                                     H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           150-152                                        13-c   C.sub.3 H.sub.7 -n                                                                     H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           161.5-162.5                                    14-c   C.sub.3 H.sub.7 -n                                                                     H  H N  OCH.sub.3                                                                           CH.sub.3                                                                           163-165                                        15-c   C.sub.3 H.sub.7 -n                                                                     H  H CH CH.sub.3                                                                            CH.sub.3                                                                           145.5-146.5                                    16-c   C.sub.4 H.sub.9 -n                                                                     H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          159-160                                        17-c   CH.sub.2 CCH                                                                           H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          172-173                                        18-c   CH.sub.2 CHCH.sub.2                                                                    H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          175.5-176.5                                    19-c   CH.sub.2 CHCH.sub.2                                                                    H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           165-166                                        20-c   C.sub.3 H.sub.7 -n                                                                     H  H CH OCHF.sub.2                                                                          OCHF.sub.2                                                                         118-119                                        21-c   CH.sub.2 CHCH.sub.2                                                                    H  H CH CH.sub.3                                                                            CH.sub.3                                                                           95-96                                          22-c   CH.sub.2 Ph                                                                            H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          159-161                                        23-c   C.sub.3 H.sub.7 -n                                                                     H  H CH OCHF.sub.2                                                                          CH.sub.3                                                                           151-152                                        25-c   C.sub.3 H.sub.7 -n                                                                     H  H CH OCHF.sub.2                                                                          Cl  225-226                                        26-c   C.sub.2 H.sub.5                                                                        H  H N  OCH.sub.3                                                                           OCH.sub.3                                                                          159-160                                        27-c   C.sub.2 H.sub.5                                                                        H  H CH OCHF.sub.2                                                                          CH.sub.3                                                                           148-149                                        28-c   C.sub.2 H.sub.5                                                                        H  H CH OCHF.sub.2                                                                          OCHF.sub.2                                                                         161-162                                        29-c   C.sub.3 H.sub.7 -n                                                                     H  H CH OCH.sub.3                                                                           OCHF.sub.2                                                                         75-77                                          30-c   C.sub.2 H.sub.5                                                                        H  H CH OCH.sub.3                                                                           OCHF.sub.2                                                                         149-151                                        31-c   C.sub.2 H.sub.5                                                                        H  H CH OCH.sub.3                                                                           Cl  141-143                                        32-c   C.sub.3 H.sub.7 -n                                                                     H  H CH OCH.sub.3                                                                           Cl  157-158                                        33-c   C.sub.2 H.sub.5                                                                        H  H CH CH.sub.3                                                                            Cl  163-164                                        34-c   C.sub.3 H.sub.7 -n                                                                     H  H CH CH.sub.3                                                                            Cl  153-156                                        35-c   CH.sub.2 CHCHCl                                                                        H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          184-185                                        36-c   CH.sub.2 CHCHCl                                                                        H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           168-169                                        38-c   CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          175.5-176.5                                    39-c   CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           151-152                                        40-c   CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H N  OCH.sub.3                                                                           CH.sub.3                                                                           148.5-149.5                                    41-c   CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H N  OCH.sub.3                                                                           OCH.sub.3                                                                          172-173                                        43-c   CH.sub.2 CHCHCl                                                                        H  H CH CH.sub.3                                                                            CH.sub.3                                                                           164-165                                        44-c   CH.sub.2 CHCHCl                                                                        H  H N  OCH.sub.3                                                                           OCH.sub.3                                                                          158-163                                        46-c   C.sub.5 H.sub.11 -n                                                                    H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          121-122                                        47-c   CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H CH CH.sub.3                                                                            CH.sub.3                                                                           154-155                                        48-c   CH.sub.2 CHCHCl                                                                        H  H CH OCH.sub.3                                                                           OCHF.sub.2                                                                         142-143                                        49-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H CH OCH.sub.3                                                                           OCH.sub.3                                                                          178-179                                        50-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H CH OCH.sub.3                                                                           CH.sub.3                                                                           159-160                                        51-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H N  OCH.sub.3                                                                           CH.sub.3                                                                           157-158                                        52-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H N  OCH.sub.3                                                                           OCH.sub.3                                                                          181-182                                        53-c   C.sub.3 H.sub.7 -n                                                                     H  H N  OC.sub.2 H.sub.5                                                                    CH.sub.3                                                                           134-135                                        54-c   C.sub.3 H.sub.7 -n                                                                     H  H N  OCH.sub.3                                                                           C.sub.2 H.sub.5                                                                    143.5-144.5                                    55-c   CH.sub.2 CHCHCl                                                                        H  H N  OC.sub.2 H.sub.5                                                                    CH.sub.3                                                                           131-133                                        56-c   CH.sub.2 CHCHCl                                                                        H  H N  OCH.sub.3                                                                           C.sub.2 H.sub.5                                                                    128-130                                        57-c   CH.sub.2 CHCHCl                                                                        H  H N  OCH.sub.3                                                                           CH.sub.2 Cl                                                                        133-135                                        58-c   C.sub.3 H.sub.7 -n                                                                     H  H N  OCH.sub.3                                                                           CH.sub.2 Cl                                                                        154-155                                        59-c   CH.sub.2 CHCHCl                                                                        H  H CH OCHF.sub.2                                                                          CH.sub.3                                                                           136-137                                        60-c   C.sub.3 H.sub.7 -n                                                                     H  H CH CF.sub.3                                                                            Cl  133-134                                        61-c   C.sub.2 H.sub.5                                                                        H  H N  OC.sub.2 H.sub.5                                                                    CH.sub.3                                                                           161-162                                        62-c   C.sub.3 H.sub.7 -n                                                                     H  H N  OCH.sub.3                                                                           C.sub.3 H.sub.7 -n                                                                 157-158                                        63-c   C.sub.3 H.sub.7 -n                                                                     H  H N  OC.sub.3 H.sub.7 -n                                                                 CH.sub.3                                                                           124-125                                        64-c   CH.sub.2 CHCHCl                                                                        H  H CH CF.sub.3                                                                            Cl  183-186                                        65-c   CH.sub.2 CHCHCl                                                                        H  H N  OCH.sub.3                                                                           C.sub.3 H.sub.7 -n                                                                 114-115                                        66-c   CH.sub.2 CHCHCl                                                                        H  H N  OC.sub.3 H.sub.7 -n                                                                 CH.sub.3                                                                           128-130                                        67-c   CH.sub.2 CHCHCl                                                                        H  H N  OCH.sub.3                                                                           CF.sub.3                                                                           138-140                                        68-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H N  OC.sub.2 H.sub.5                                                                    CH.sub.3                                                                           139-140                                        69-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H N  OCH.sub.3                                                                           C.sub.2 H.sub.5                                                                    149-150                                        70-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H N  OCH.sub.3                                                                           CF.sub.3                                                                           152-154                                        71-c   CH.sub.2 C(Cl)CH.sub.2                                                                 H  H CH OCH.sub.3                                                                           OCHF.sub.2                                                                         86-87                                          __________________________________________________________________________

                  TABLE 14c-2                                                      ______________________________________                                          ##STR763##                                                                    Compound                                     m.p.                              No.     R.sup.c1                                                                              R.sup.c4                                                                             R.sup.c5                                                                           R.sup.c6                                                                           A   B     D     (°C.)                      ______________________________________                                         8-c     C.sub.2 H.sub.5                                                                       H     H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            189-190                           9-c     C.sub.2 H.sub.5                                                                       H     H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             165-166                           10-c    C.sub.2 H.sub.5                                                                       H     H   H   CH  CH.sub.3                                                                             CH.sub.3                                                                             178-179                           ______________________________________                                    

                  TABLE 14c-3                                                      ______________________________________                                          ##STR764##                                                                    Compound                                   m.p.                                No.     R.sup.c1                                                                              R.sup.c7                                                                              R.sup.c8                                                                            A   B     D     (°C.)                        ______________________________________                                         42-c    CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.3                                                                            CH  OCH.sub.3                                                                            OCH.sub.3                                                                            180-192                                                                        (decom-                                                                        posed)                              ______________________________________                                    

EXAMPLE d-1 Preparation of 1-(3-methylthiazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR765##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was further stirred at the same temperature for 10 minutes. The reaction mixture was cooled again to -30° C., and a mixture comprising 2.84 g (11 mmol) of 3-methyl-2-iminothiazolidin-4-one hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 20 minutes. Then, the solvent was distilled off under reduced pressure, and then 100 ml of water was added to the obtained residue. Precipitated crystals were extracted three times with 100 ml of chloroform. The chloroform layer was washed with water and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethyl ether/acetonitrile and collected by filtration to obtain 1.5 g of desired 1-(3-methylthiazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea as colorless crystals.

Melting point: 200°-201° C.

EXAMPLE d-2 Preparation of 1-(1-methyl-3-n-propylimidazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR766##

1.16 9 (7.5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20 ml of dry tetrahydrofuran, and 1.07 g (7.5 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -40° C. The reaction temperature was raised to 0° C., and then the reaction mixture was cooled again to -40° C. Then, a mixture comprising 1.16 g (7.5 mmol) of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one, 0.83 g (8.2 mmol) of triethylamine and 20 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 2 hours. Then, the solvent was distilled off under reduced pressure, and then 100 ml of water was added to the obtained residue. The mixture was extracted three times with 100 ml of chloroform. Then, the chloroform layer was washed with water and then dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and precipitated crystals were washed with a solvent mixture of ethyl ether/acetonitrile and collected by filtration to obtain 0.16 g of desired 1-(1-methyl-3-n-propylimidazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 96°-98° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples d-1 and d-2 are presented in Table 14d.

                                      TABLE 14d                                    __________________________________________________________________________      ##STR767##                                                                    Compound                      m.p.                                             No.   R.sup.d1                                                                              R.sup.d4                                                                          R.sup.d5                                                                          A  B   D   (°C.)                                     __________________________________________________________________________     3-d   CH.sub.3                                                                              H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          188-189                                          4-d   C.sub.2 H.sub.5                                                                       H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          111-113                                          5-d   CH.sub.2 CHCH.sub.2                                                                   H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          156-158                                          6-d   CH.sub.2 CCH                                                                          H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          181-182                                          7-d   CH.sub.2 COCH.sub.3                                                                   H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          190-192                                          8-d   CH.sub.2 CO.sub.2 CH.sub.3                                                            H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          188-190                                          9-d   CH.sub.2 OCH.sub.3                                                                    H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          155-156                                          10-d  CH.sub.2 SCH.sub.3                                                                    H  CH.sub.3                                                                          CH OCH.sub.3                                                                          OCH.sub.3                                                                          115-120                                                                        (decom-                                                                        posed)                                           __________________________________________________________________________

EXAMPLE e-1 Preparation of 1-(3,6-dihydro-3-n-propyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR768##

0.32 g (2.06 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and the solution was cooled to -40° C. At the same temperature, 0.29 g (2.05 mmol) of chlorosulfonyl isocyanate was dropwise added thereto. Then, the temperature was raised to 0° C. The mixture was cooled again to -40° C., and then a mixed solution comprising 0.4 g (2.56 mmol) of 3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine, 0.26 g (2.57 mmol) of triethylamine and 40 ml of dry tetrahydrofuran, was dropwise added thereto. The mixture was gradually heated to room temperature with stirring, and then the solvent was distilled off under reduced pressure. 100 ml of water was added to the residue, and then the mixture was extracted twice with 50 ml of chloroform. The chloroform layer was washed with water and then dried over anhydrous sodium sulfate. Then, chloroform was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile and then with ethyl ether to obtain 0.3 g of desired 1-(3,6-dihydro-3-n-propyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 161°-163° C.

EXAMPLE e-2 Preparation of 1-(3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR769##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -15° C. to -5° C. The reaction solution was heated to 0° C. and then further stirred at the same temperature for 15 minutes. Then, the reaction solution was cooled again to -30° C., and a mixed solution comprising 1.56 g (12 mmol) of 3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine, 1.21 g (12 mmol) of triethylamine and 10 ml of dry tetrahydrofuran, was dropwise added thereto. The reaction solution was gradually heated to room temperature with stirring, and then the solvent was distilled off under reduced pressure. 80 ml of water was added to the residue, and precipitated crystals were extracted three times with 60 ml of chloroform. The chloroform layer was washed with water and dried over anhydrous sodium sulfate. Then, chloroform was distilled off under reduced pressure.

Obtained crystals were washed with a solvent mixture of ethyl ether/acetonitrile to obtain 1.2 g of desired 1-(3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 188°-190° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples e-1 and e-2 are presented in Tables 14e-1 and 14e-2.

                  TABLE 14e-1                                                      ______________________________________                                          ##STR770##                                                                    Com-                                                                           pound                                        m.p.                              No.   R.sup.e1 R.sup.e2                                                                             R.sup.e3                                                                           R.sup.e4                                                                           A   B     D     (°C.)                      ______________________________________                                         3-e   CH.sub.3 H     H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            194-196                           4-e   CH.sub.2 OCH.sub.3                                                                      H     H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            158-160                           ______________________________________                                    

                  TABLE 14e-2                                                      ______________________________________                                          ##STR771##                                                                    Com-                                                                           pound                                        m.p.                              No.   R.sup.e1                                                                               R.sup.e8                                                                             R.sup.e9                                                                           R.sup.e10                                                                           A   B     D     (°C.)                      ______________________________________                                         5-e   C.sub.3 H.sub.7 -n                                                                     H     H   H    CH  OCH.sub.3                                                                            OCH.sub.3                                                                            166-167                           ______________________________________                                    

EXAMPLE f-1 Preparation of 1-(3-methyloxazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)ure ##STR772##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -20° C. The reaction temperature was raised to -5° C., and the mixture was stirred at the same temperature for 5 minutes. The reaction mixture was cooled again to -20° C., and a mixture comprising 2.28 g (10 mmol) of 2-imino-3-methyloxazolidine hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and then 100 ml of water was added to the obtained residue. Precipitated crystals were collected by filtration, washed with water and then with a solvent mixture of ethyl ether/acetonitrile and dried to obtain 0.8 g of desired 1-(3-methyloxazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 174°-175° C.

The structures and the physical property values of the compounds prepared by the same method as in Example f-1 are presented in Tables 14f.

                  TABLE 14f                                                        ______________________________________                                          ##STR773##                                                                    Com-                                                                           pound                                       m.p.                               No.    R.sup.f1   R.sup.f5                                                                             R.sup.f6                                                                           A   B     D     (°C.)                       ______________________________________                                         2-f    CH.sub.2 CHCH.sub.2                                                                       H     H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            157-159                            ______________________________________                                    

EXAMPLE g-1 Preparation of 1- N-((methylthio-N,N-dimethylamino)methylene)aminosulfonyl!-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR774##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was cooled again to -20° C. Then, a mixture comprising 2.5 g (10.2 mmol) of N,N-dimethyl-S-methylisothiourea hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 10 minutes. Then, the solvent was distilled off under reduced pressure, and then 80 ml of water was added to the obtained residue. The mixture was extracted three times with 30 ml of chloroform. The chloroform layer was washed with water and then dried over anhydrous sodium sulfate. Then, solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethyl ether/acetonitrile to obtain 2 g of desired 1- N-((methylthio-N,N-dimethylamino)methylene)aminosulfonyl!-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 167°-168° C.

EXAMPLE g-2 Preparation of 1- N-((methylthio-N-ethyl-N-methylamino)methylene)aminosulfonyl!-3-(4,6-dimethoxypyrimidin-2-yl)urea ##STR775##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was cooled again to -20° C. Then, a mixture comprising 2.60 g (10 mmol) of N-ethyl-N-methyl-S-methylisothiourea hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and 80 ml of water was added to the obtained residue. The mixture was extracted three times with 50 ml of chloroform. The chloroform layer was washed with water, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile to obtain 1.32 g of desired 1- N-((methylthio-N-ethyl-N-methylamino)methylene)aminosulfonyl!-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 143°-144° C.

EXAMPLE g-3 Preparation of 1- N-((methylthio-N-methoxy-N-methylaminomethylene)aminosulfonyl!-3-4,6-dimethoxypyrimidin-2-yl)urea ##STR776##

0.78 g (5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20 ml of dry tetrahydrofuran, and 0.71 g (5 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to -20° C. Then, a mixture comprising 1.31 g (5 mmol) of N-methoxy-N-methyl-S-methylisothiourea hydroiodide, 1.11 g (11 mmol) of triethylamine and 15 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and then 40 ml of water was added to the obtained residue. The mixture was extracted three times with 25 ml of chloroform. The chloroform layer was washed with water, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile to obtain 1.51 g of desired 1- N-((methylthio-N-methoxy-N-methylamino)methylene)aminosulfonyl!-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 165°-167° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples g-1 to g-3 are presented in Table 14g.

                                      TABLE 14g                                    __________________________________________________________________________      ##STR777##                                                                    Compound                         m.p.                                          No.   R.sup.g1                                                                              R.sup.g2                                                                          R.sup.g3                                                                              A B   D   (°C.)                                  __________________________________________________________________________      2-g  C.sub.2 H.sub.5                                                                       CH.sub.3                                                                          CH.sub.3                                                                              CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          129-130                                        3-g  C.sub.3 H.sub.7 -n                                                                    CH.sub.3                                                                          CH.sub.3                                                                              CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          115-116                                        4-g  CH.sub.2 CHCH.sub.2                                                                   CH.sub.3                                                                          CH.sub.3                                                                              CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          131-132                                        5-g  CH.sub.2 CCH                                                                          CH.sub.3                                                                          CH.sub.3                                                                              CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          140-141                                        6-g  CH.sub.3                                                                              CH.sub.3                                                                          COCH.sub.3                                                                            CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          162-164                                        8-g  CH.sub.3                                                                              (CH.sub.2).sub.4                                                                         CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          184-186                                        9-g  CH.sub.3                                                                              CH.sub.3                                                                          C.sub.3 H.sub.7 -n                                                                    CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          123-125                                       10-g  CH.sub.3                                                                              CH.sub.3                                                                          Ph     CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          163-164                                       11-g  CH.sub.3                                                                              CH.sub.3                                                                          CH.sub.3                                                                              CH                                                                               OCH.sub.3                                                                          CH.sub.3                                                                           178-179                                       13-g  CH.sub.3                                                                              CH.sub.3                                                                          OC.sub.2 H.sub.5                                                                      CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          142-143                                       14-g  CH.sub.3                                                                              CH.sub.3                                                                          OC.sub.3 H.sub.7 -n                                                                   CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          124-125                                       15-g  CH.sub.3                                                                              CH.sub.3                                                                          OC.sub.3 H.sub.7 -n                                                                   CH                                                                               OCH.sub.3                                                                          CH.sub.3                                                                           142-143                                       16-g  CH.sub.3                                                                              CH.sub.3                                                                          OC.sub.2 H.sub.5                                                                      CH                                                                               OCH.sub.3                                                                          CH.sub.3                                                                           141-142                                       17-g  CH.sub.3                                                                              CH.sub.3                                                                          OC.sub.2 H.sub.5                                                                      N OCH.sub.3                                                                          CH.sub.3                                                                           148-149                                       18-g  CH.sub.3                                                                              CH.sub.3                                                                          OC.sub.3 H.sub.7 -n                                                                   N OCH.sub.3                                                                          CH.sub.3                                                                           138-139                                       19-g  CH.sub.3                                                                              CH.sub.3                                                                          CH.sub.2 CHCH.sub.2                                                                   CH                                                                               OCH.sub.3                                                                          OCH.sub.3                                                                          138-141                                       20-g  CH.sub.3                                                                              CH.sub.3                                                                          CH.sub.3                                                                              N OCH.sub.3                                                                          CH.sub.3                                                                           166-167                                       __________________________________________________________________________

Now, Formulation Examples of the herbicides containing the compounds of the present invention will be given specifically. However, it should be understood that the present invention is by no means restricted to such specific Examples. In the following Formulation Examples, "parts" means "parts by weight".

    ______________________________________                                         Wettable powder                                                                ______________________________________                                         Compound of the present invention                                                                      5-80    parts                                          Solid carrier           10-85   parts                                          Surfactant              1-10    parts                                          Other                   1-5     parts                                          ______________________________________                                    

As other, a coagulation preventing agent may, for example, be mentioned.

    ______________________________________                                         Emulsifiable concentrate                                                       Compound of the present invention                                                                      1-30    parts                                          Liquid carrier          30-95   parts                                          Surfactant              5-15    parts                                          Flowable                                                                       Compound of the present invention                                                                      5-70    parts                                          Liquid carrier          15-65   parts                                          Surfactant              5-12    parts                                          Other                   5-30    parts                                          ______________________________________                                    

As other, an antifreezing agent and a thickener may, for example, be mentioned.

    ______________________________________                                         Granular wettable powder (dry flowable)                                        Compound of the present invention                                                                       20-90   parts                                         Solid carrier            10-60   parts                                         Surfactant               1-20    parts                                         Granule                                                                        Compound of the present invention                                                                       0.1-10  parts                                         Solid carrier            90-99.9 parts                                         Other                    1-5     parts                                         FORMULATION EXAMPLE a-1: Wettable powder                                       Compound No. 1-a of the present invention                                                               20      parts                                         Zeeklite A (tradename for a kaolin-type                                                                 76      parts                                         clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2       parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   2       parts                                         preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE a-2: Wettable powder                                       ______________________________________                                         Compound No. 2-a of the present invention                                                               40      parts                                         Zeeklite A (tradename for a kaolin-type                                                                 54      parts                                         clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2       parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   4       parts                                         preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE a-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 3-a of the present invention                                                               5       parts                                         Xylene                   75      parts                                         N,N-dimethylformamide    15      parts                                         Sorpol 2680 (tradename for a mixture of a                                                               5       parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE a-4: Flowable                                              ______________________________________                                         Compound No. 7-a of the present invention                                                               25      parts                                         Agrizole S-710 (tradename for a nonionic                                                                10      parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5     part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20      parts                                         manufactured by Rhone-Poulenc)                                                 Water                    44.5    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE a-5: Flowable                                              ______________________________________                                         Compound No. 8-a of the present invention                                                               40      parts                                         Agrizole S-710 (tradename for a nonionic                                                                10      parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5     part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20      parts                                         manufactured by Rhone-Poulenc)                                                 Water                    29.5    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE a-6: Granular wettable powder                              (dry flowable)                                                                 ______________________________________                                         Compound No. 10-a of the present invention                                                              75      parts                                         Isoban No. 1 (tradename for an anionic                                                                  10      parts                                         surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                     5       parts                                         surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                              10      parts                                         manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE a-7: Granule                                               ______________________________________                                         Compound No. 69-a of the present invention                                                              1       part                                          Bentonite                55      parts                                         Talc                     44      parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE b-1: Wettable powder                                       ______________________________________                                         Compound No. 1-b of the present invention                                                               20      parts                                         Zeeklite A (tradename for a kaolin-type                                                                 76      parts                                         clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2       parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   2       parts                                         preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE b-2: Wettable powder                                       ______________________________________                                         Compound No. 2-b of the present invention                                                               40      parts                                         Zeeklite A (tradename for a kaolin-type                                                                 54      parts                                         clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2       parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Cheinical                                     Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   4       parts                                         preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE b-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 3-b of the present invention                                                               5       parts                                         Xylene                   75      parts                                         N,N-dimethylformamide    15      parts                                         Sorpol 2680 (tradename for a mixture of a                                                               5       parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE b-4: Flowable                                              ______________________________________                                         Compound No. 1-b of the present invention                                                               25      parts                                         Agrizole S-710 (tradename for a nonionic                                                                10      parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5     part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20      parts                                         manufactured by Rhone-Poulenc)                                                 Water                    44.5    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE b-5: Flowable                                              ______________________________________                                         Compound No. 4-b of the present invention                                                               40      parts                                         Agrizole S-710 (tradename for a nonionic                                                                10      parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5     part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20      parts                                         manufactured by Rhone-Poulenc)                                                 Water                    29.5    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE b-6: Granular wettable powder (dry                         flowable)                                                                      ______________________________________                                         Compound No. 5-b of the present invention                                                              75 parts                                               Isoban No. 1 (tradename for an anionic                                                                 10 parts                                               surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                     5 parts                                               surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                             10 parts                                               manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE b-7: Granule                                               ______________________________________                                         Compound No. 6-b of the present invention                                                                 1 part                                              Bentonite                 55 parts                                             Talc                      44 parts                                             ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE c-1: Wettable powder                                       ______________________________________                                         Compound No. 1-c of the present invention                                                              20 parts                                               Zeeklite A (tradename for a kaolin-type                                                                76 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   2 parts                                               preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE c-2: Wettable powder                                       ______________________________________                                         Compound No. 2-c of the present invention                                                              40 parts                                               Zeeklite A (tradename for a kaolin-type                                                                54 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   4 parts                                               preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        CO., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE c-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 12-c of the present invention                                                              5 parts                                               Xylene                  75 parts                                               N,N-dimethylformamide   15 parts                                               Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE c-4: Flowable                                              ______________________________________                                         Compound No. 24-c of the present invention                                                               25 parts                                             Agrizole S-710 (tradename for a nonionic                                                                 10 parts                                             surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5 part                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20 parts                                             manufactured by Rhone-Poulenc)                                                 Water                     44.5 parts                                           ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE c-5: Flowable                                              ______________________________________                                         Compound No. 37-c of the present invention                                                               40 parts                                             Agrizole S-710 (tradename for a nonionic                                                                 10 parts                                             surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5 part                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20 parts                                             manufactured by Rhone-Poulenc)                                                 Water                     29.5 parts                                           ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE c-6: Granular wettable powder (dry                         flowable)                                                                      ______________________________________                                         Compound No. 45-c of the present invention                                                             75 parts                                               Isoban No. 1 (tradename for an anionic                                                                 10 parts                                               surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                     5 parts                                               surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                             10 parts                                               manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE c-7: Granule                                               ______________________________________                                         Compound No. 48-c of the present invention                                                                1 part                                              Bentonite                 55 parts                                             Talc                      44 parts                                             ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE d-1: Wettable powder                                       ______________________________________                                         Compound No. 1-d of the present invention                                                              20 parts                                               Zeeklite A (tradename for a kaolin-type                                                                76 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   2 parts                                               preventing agent composed of a white carbon                                    manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE d-2: Wettable powder                                       ______________________________________                                         Compound No. 2-d of the present invention                                                              40 parts                                               Zeeklite A (tradename for a kaolin-type                                                                54 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   4 parts                                               preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE d-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 3-d of the present invention                                                               5 parts                                               Xylene                  75 parts                                               N,N-dimethylformamide   15 parts                                               Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE d-4: Flowable                                              ______________________________________                                         Compound No. 4-d of the present invention                                                                25 parts                                             Agrizole S-710 (tradename for a nonionic                                                                 10 parts                                             surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5 part                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20 parts                                             manufactured by Rhone-Poulenc)                                                 Water                     44.5 parts                                           ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE d-5: Flowable                                              ______________________________________                                         Compound No. 5-d of the present invention                                                                40 parts                                             Agrizole S-710 (tradename for a nonionic                                                                 10 parts                                             surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5 part                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20 parts                                             manufactured by Rhone-Poulenc)                                                 Water                     29.5 parts                                           ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE d-6: Granular wettable powder (dry                         flowable)                                                                      ______________________________________                                         Compound No. 6-d of the present invention                                                              75 parts                                               Isoban No. 1 (tradename for an anionic                                                                 10 parts                                               surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                     5 parts                                               surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                             10 parts                                               manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE d-7: Granule                                               ______________________________________                                         Compound No. 9-d of the present invention                                                                1     part                                           Bentonite                 55    parts                                          Talc                      44    parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE e-1: Wettable powder                                       ______________________________________                                         Compound No. 1-e of the present invention                                                              20 parts                                               Zeeklite A (tradename for a kaolin-type                                                                76 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   2 parts                                               preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE e-2: Wettable powder                                       ______________________________________                                         Compound No. 2-e of the present invention                                                              40 parts                                               Zeeklite A (tradename for a kaolin-type                                                                54 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   4 parts                                               preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE e-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 3-e of the present invention                                                               5 parts                                               Xylene                  75 parts                                               N,N-dimethylformamide   15 parts                                               Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE e-4: Flowable                                              ______________________________________                                         Compound No. 4-e of the present invention                                                               25     parts                                          Agrizole S-710 (tradename for a nonionic                                                                10     parts                                          surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5    part                                           surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20     parts                                          manufactured by Rhone-Poulenc)                                                 Water                    44.5   parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE e-5: Flowable                                              ______________________________________                                         Compound No. 5-e of the present invention                                                               40     parts                                          Agrizole S-710 (tradename for a nonionic                                                                10     parts                                          surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5    part                                           surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20     parts                                          manufactured by Rhone-Poulenc)                                                 Water                    29.5   parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE e-6: Granular wettable powder (dry                         flowable)                                                                      ______________________________________                                         Compound No. 1-e of the present invention                                                              75 parts                                               Isoban No. 1 (tradename for an anionic                                                                 10 parts                                               surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                     5 parts                                               surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                             10 parts                                               manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE e-7: Granule                                               ______________________________________                                         Compound No. 5-e of the present invention                                                              1 part                                                 Bentonite               55 parts                                               Talc                    44 parts                                               ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE f-1: Wettable powder                                       ______________________________________                                         Compound No. 1-f of the present invention                                                              20 parts                                               Zeeklite A (tradename for a kaolin-type                                                                76 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   2 parts                                               preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE f-2: Wettable powder                                       ______________________________________                                         Compound No. 2-f of the present invention                                                              40 parts                                               Zeeklite A (tradename for a kaolin-type                                                                54 parts                                               clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                               2 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                   4 parts                                               preventing agent composed of a white carbon,                                   manufactured by Shionogi pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE f-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 1-f of the present invention                                                               5 parts                                               Xylene                  75 parts                                               N,N-dimethylformamide   15 parts                                               Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                               nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE f-4: Flowable                                              ______________________________________                                         Compound No. 2-f of the present invention                                                               25     parts                                          Agrizole S-710 (tradename for a nonionic                                                                10     parts                                          surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5    part                                           surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20     parts                                          manufactured by Rhone-Poulenc)                                                 Water                    44.5   parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE f-5: Flowable                                              ______________________________________                                         Compound No. 2-f of the present invention                                                               40     parts                                          Agrizole S-710 (tradename for a nonionic                                                                10     parts                                          surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5    part                                           surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20     parts                                          manufactured by Rhone-Poulenc)                                                 Water                    29.5   parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE f-6: Granular wettable powder (dry                         flowable)                                                                      ______________________________________                                         Compound No. 2-f of the present invention                                                              75 parts                                               Isoban No. 1 (tradename for an anionic                                                                 10 parts                                               surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                     5 parts                                               surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                             10 parts                                               manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE f-7: Granule                                               ______________________________________                                         Compound No. 2-f of the present invention                                                                1     part                                           Bentonite                 55    parts                                          Talc                      44    parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE g-1: Wettable powder                                       ______________________________________                                         Compound No. 1-g of the present invention                                                                20    parts                                          Zeeklite A (tradename for a kaolin-type                                                                  76    parts                                          clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                2     parts                                          nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                    2     parts                                          preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE g-2: Wettable powder                                       ______________________________________                                         Compound No. 2-g of the present invention                                                                40    parts                                          Zeeklite A (tradename for a kaolin-type                                                                  54    parts                                          clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                2     parts                                          nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chernical                                     Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                    4     parts                                          preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE g-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 3-g of the present invention                                                                5     parts                                          Xylene                    75    parts                                          N,N-dimethylformamide     15    parts                                          Sorpol 2680 (tradename for a mixture of a                                                                5     parts                                          nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE g-4: Flowable                                              ______________________________________                                         Compound No. 4-g of the present invention                                                               25     parts                                          Agrizole S-710 (tradename for a nonionic                                                                10     parts                                          surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5    part                                           surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20     parts                                          manufactured by Rhone-Poulenc)                                                 Water                    44.5   parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE g-5: Flowable                                              ______________________________________                                         Compound No. 5-g of the present invention                                                               40     parts                                          Agrizole S-710 (tradename for a nonionic                                                                10     parts                                          surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                   0.5    part                                           surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                            20     parts                                          manufactured by Rhone-Poulenc)                                                 Water                    29.5   parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE g-6: Granular wettable powder (dry                         flowable)                                                                      ______________________________________                                         Compound No. 12-g of the present invention                                                               75    parts                                          Isoban No. 1 (tradenarne for an anionic                                                                  10    parts                                          surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                      5     parts                                          surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                               10    parts                                          manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE g-7: Granule                                               ______________________________________                                         Compound No. 19-g of the present invention                                                               1     part                                           Bentonite                 55    parts                                          Talc                      44    parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

In use, the above wettable powder, emulsifiable concentrate, flowable or granular wettable powder is diluted with water from 50 to 1,000 times and applied so that the active ingredient will be from 0.0001 to 10 kg per hectare (ha).

Now, the herbicidal activities of the compounds of the present invention will be described in detail with reference to the following Test Examples.

TEST EXAMPLE 1

Test-1 on the herbicidal effects in soil treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Digitaria adscendens, Cyperus microiria, Solanum nigrum, Galinsoga ciliata, Rorippa indica, Oryza sativa, Zea mays, Triticum aestivum, Glycine max and Gossypium spp. were sown, and the soil was covered thereon in a thickness of about 1.5 cm, and then a herbicide solution was applied onto the surface of the soil uniformly so that the active ingredient was distributed at a predetermined concentration. The herbicide solution was prepared by diluting a wettable powder prepared in accordance with the foregoing Formulation Examples with water and applied by a small spray onto the entire soil surface. Four weeks after the application of the herbicidal solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were determined on the basis of the following standard ratings. The results are shown in Table 15.

Standard ratings:

5: Growth control rate of more than 90% (almost completely withered)

4: Growth control rate of from 70 to 90%

3: Growth control rate of from 40 to 70%

2: Growth control rate of from 20 to 40%

1: Growth control rate of from 5 to 20%

0: Growth control rate of less than 5% (almost non-effective)

The above growth control rates were calculated by the following equation:

    Growth control rate (%)=(1-T/N)×100

where

T: Weight of the weed grown above the soil surface of the treated area

N: Weight of the weed grown above the soil surface of the non-treated area

TEST EXAMPLE 2

Test-1 on the herbicidal effects in foliage treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Digitaria adscendens, Avena fatua, Cyperus microiria, Solanum nigrum, Galinsoga ciliata, Rorippa indica, Oryza sativa, Zea mays, Triticum aestivum, Glycine max, Gossypium spp. and Beta vulgaris were spot-wisely sown, and the soil was covered thereon in a thickness of about 1.5 cm. When the various weeds and crop plants grew to the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient was applied in a predetermined concentration. The herbicidal solution was prepared by diluting a wettable powder prepared in accordance with the above Formulation Examples with water and applied onto the entire surface of the foliages of the weeds and the crop plants by a small spray. Four weeks after the application of the herbicide solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were determined on the basis of the standard ratings described in Test Example 1. The results are shown in Table 16.

TEST EXAMPLE 3

Test-1 on the herbicidal effects in irrigation treatment

Into a Wagner pot of 1/5000a, alluvial soil was put, and then water was introduced and mixed to form an irrigated state with a water depth of 4 cm. Seeds of Echinochloa crus-galli, Scirpus juncoides, Monochoria vaginalis and Rotala indica were sown in the above pot, and tubers of Sagittaria pygmaea and Cyperus serotinus were embedded. Then, rice seedlings of 2.5 leaf stage were transplanted. The pot was placed in a greenhouse at a temperature of from 25° to 30° C., and the plants were cultured. On the third day after the seeding and plantation, a diluted solution of the herbicide was dropwise applied to the water surface by a measuring pipette, so that the dose would be a predetermined level. Three weeks after the dropwise application of the herbicide, the herbicidal effects against various weeds and rice were determined on the basis of the standard ratings described in Test Example 1. The results are shown in Table 17.

In Tables 15, 16 and 17, Compound Nos. correspond to Compound Nos. in the Examples, and symbols have the following meanings.

A: Echinochloa crus-galli (barnyardgrass)

B: Digitaria adscendens (large crabgrass)

C: Arena fatua (wild oat)

D: Cyperus microiria (annual sedge)

E: Solanum nigrum (black nightshade)

F: Galinsoga ciliata (hairy galinsoga)

G: Rorippa indica (fieldcress)

H: Scirpus juncoides (bulrush)

I: Monochoria vaginalis (ducksalad)

J: Rotala indica (toothcup)

K: Sagittaria pygmaea (arrowhead)

L: Cyperus serotinus (flat sedge)

a: Oryza sativa (rice)

b: Zea mays (corn)

c: Triticum aestivum (wheat)

d: Glycine max (soybean)

e: Gossypium spp. (cotton)

f: Beta vulgaris (sugar beet)

                  TABLE 15                                                         ______________________________________                                              Dose                                                                                                   No. (kg/ha) A B D E F G a b c d e                 ______________________________________                                         1-a  2.5     4      4   5   1   3   5    5   5   5   4                                                      3                                                                              2-a 0.04 5 5 5 1 5 5 1 0 0 0 0                                                  0.08 5 5 5 1 5 5 2 1 1 0 0                                                     0.16 5 5 5 2 5 5 3 3 2 1 0                                                    3-a 2.5 4 4 1 1 0 4 3 0 2 1 0                                                  6-a 0.63 5 5 5 0 4 4 4 1 3 0 0                                                 7-a 0.04 4 5 5 0 3 4 0 0 0 0 0                                                  0.08 5 5 5 0 4 5 0 0 0 0 0                                                     0.16 5 5 5 2 5 5 2 0 0 0 0                                                    8-a 0.63 5 5 5 2 5 5 3 0 0 0 0                                                 10-a 0.16 4 5 5 0 2 4 0 0 0 0 0                                                 0.32 5 5 5 0 4 5 1 0 0 0 0                                                     0.63 5 5 5 0 5 5 3 0 0 0 0                                                    12-a 0.04 5 4 4 0 3 5 0 0 0 0                                                   0.08 5 5 5 0 4 5 1 0 0 0 0                                                     0.16 5 5 5 1 5 5 3 1 0 0 0                                                    20-a 0.04 4 2 5 0 3 3 1 0 0 0 0                                                 0.08 5 3 5 0 4 4 2 0 0 0 0                                                     0.16 5 4 5 1 5 5 3 1 0 0 0                                                    22-a 0.16 5 2 5 0 5 5 0 0 0 0 0                                                 0.32 5 3 5 1 5 5 0 0 0 0 0                                                     0.63 5 4 5 1 5 5 1 0 0 0 0                                                    24-a 0.16 5 5 4 0 3 4 0 0 0 0 0                                                 0.32 5 5 5 0 4 5 2 0 0 0 0                                                     0.63 5 5 5 0 5 5 3 1 1 0 0                                                    25-a 0.63 5 5 5 2 4 5 3 1 1 0 0                                                26-a 0.63 4 3 4 0 4 5 0 0 0 0 0                                                30-a 2.5 3 2 5 4 5 5 4 3 2 1 0                                                 31-a 2.5 2 2 5 4 4 5 2 0 1 0 0                                                 34-a 2.5 5 5 5 4 5 5 3 3 5 0 0                                                 36-a 2.5 5 4 5 5 5 5 1 0 0 0 0                                                 38-a 0.63 5 5 5 2 4 5 2 1 0 0 0                                                39-a 2.5 5 5 5 4 4 5 3 1 0 0 0                                                 40-a 0.63 5 5 5 3 4 5 2 1 1 0 0                                                41-a 2.5 5 5 5 4 5 5 4 4 1 1 0                                                 43-a 2.5 3 4 5 3 3 5 0 0 0 0 0                                                 45-a 0.63 5 5 5 0 5 5 0 0 0 0 0                                                47-a 0.63 5 4 5 3 5 5 3 3 1 0 0                                                48-a 0.63 5 4 5 1 5 5 5 3 2 0 0                                                49-a 2.5 5 5 5 2 5 5 3 2 1 0 0                                                 52-a 2.5 5 5 5 3 3 5 4 1 1 0 0                                                 53-a 2.5 5 5 5 3 3 5 5 0 0 0 0                                                 56-a 2.5 5 5 5 3 5 5 4 3 3 3 0                                                 59-a 0.63 5 4 5 5 5 5 1 0 0 0 0                                                61-a 2.5 5 5 5 4 5 5 1 2 1 0 0                                                 63-a 0.63 5 5 5 3 5 5 3 1 2 0 0                                                64-a 2.5 5 5 5 2 5 5 3 2 3 1 0                                                 73-a 0.63 5 5 5 3 5 5 5 5 5 3 0                                                74-a 0.63 5 5 5 2 5 5 3 2 2 0 0                                                1-b 5 -- -- 4 -- 3 5 -- 0 0 0 --                                               3-b 5 -- -- 3 -- 2 4 -- 0 0 0 --                                               1-c 0.16 5 5 5 2 4 5 5 4 1 4 0                                                 2-c 0.16 5 5 5 4 5 5 5 4 2 0 0                                                 3-c 0.16 5 5 5 2 5 5 5 3 3 1 0                                                 4-c 0.63 4 5 5 2 4 5 1 1 0 0 0                                                 5-c 0.63 5 5 5 1 5 5 1 0 0 0 0                                                 6-c 0.63 2 3 5 0 4 5 1 0 0 0 0                                                 7-c 0.63 5 5 5 2 5 5 4 1 0 1 0                                                 8-c 10 2 4 5 5 4 5 1 0 0 0 0                                                   11-c 0.63 5 5 5 2 5 5 3 2 1 0 0                                                12-c 0.16 5 5 5 2 5 5 4 2 0 0 0                                                13-c 0.16 5 5 5 4 5 5 4 3 3 0 0                                                14-c 0.63 5 5 5 0 5 5 2 0 0 0 0                                                15-c 0.63 5 5 5 3 5 5 2 1 0 0 0                                                16-c 0.63 5 5 5 4 5 5 4 4 3 0 0                                                17-c 0.63 5 5 5 3 5 5 2 0 0 0 0                                                18-c 0.16 5 5 5 3 5 5 5 2 0 0 0                                                20-c 0.63 0 0 3 3 5 5 0 0 0 0 0                                                23-c 0.63 4 3 5 5 5 5 5 1 2 0 0                                                24-c 0.16 5 5 1 2 5 5 4 1 1 0 0                                                26-c 0.63 5 5 4 2 5 5 5 3 5 3 0                                                35-c 0.16 5 5 5 3 5 5 5 5 4 0 0                                                36-c 0.16 5 5 5 3 5 5 5 4 4 0 0                                                37-c 0.16 5 5 5 4 5 5 5 5 5 4 1                                                38-c 0.63 5 5 5 3 5 5 5 5 2 0 1                                                39-c 0.63 5 5 5 3 5 5 4 4 3 1 0                                                40-c 0.16 5 5 5 4 5 5 5 5 5 2 2                                                2-d 2.5 4 5 5 5 4 5 0 0 0 0 0                                                  3-d 2.5 5 5 5 5 0 5 0 0 0 0 0                                                  5-d 2.5 3 5 5 5 3 5 3 0 0 0 0                                                  6-d 10 2 4 5 5 5 5 1 0 0 0 1                                                   9-d 10 3 5 5 5 5 5 3 1 1 0 0                                                   1-e 5 5 5 5 2 2 5 5 1 0 0 0                                                    2-e 2.5 3 3 2 1 0 2 0 0 0 0 0                                                  4-e 5 3 5 5 3 3 5 1 0 0 0 0                                                    2-f 10 4 5 5 5 5 5 4 0 1 0 0                                                   1-g 0.63 5 5 5 5 5 5 3 0 1 1 0                                                 7-g 2.5 5 5 5 3 5 5 3 1 4 2 1                                                  9-g 2.5 5 5 5 5 5 5 0 0 0 0 0                                                  11-g 0.63 5 5 5 3 5 5 3 2 1 1 0                                                12-g 2.5 5 4 5 3 5 5 1 1 1 0 0                                                 13-g 2.5 5 3 5 3 5 5 1 0 1 0 0                                                 14-g 2.5 4 4 5 3 5 5 0 0 0 0 0                                                 15-g 2.5 5 4 5 3 5 5 1 1 2 0 0                                                 16-g 2.5 5 4 5 3 5 5 3 3 4 0 0                                                 17-g 0.63 5 5 5 5 5 5 3 1 3 0 0                                                18-g 0.63 5 5 5 5 5 5 4 2 2 0 0                                                19-g 2.5 4 5 5 2 5 5 4 3 3 1 0                    ______________________________________                                    

                                      TABLE 16                                     __________________________________________________________________________        Dose                                                                        No.                                                                               (kg/ha)                                                                            A  B C  D E  F G a  b c  d  e f                                         __________________________________________________________________________     1-a                                                                               2.5 4  2 4  2 5  4 4 3  3 3  3  1 3                                         2-a                                                                               0.16                                                                               5  2 4  3 4  4 4 2  3 2  3  0 1                                            0.32                                                                               5  3 5  4 5  5 5 2  4 2  3  1 2                                            0.63                                                                               5  3 5  4 5  5 5 3  4 3  4  2 2                                         3-a                                                                               2.5 4  3 4  2 3  1 2 1  1 2  3  1 1                                         6-a                                                                               2.5 5  3 5  2 3  3 4 4  4 3  3  1 0                                         7-a                                                                               0.16                                                                               5  1 3  2 3  2 3 1  3 0  0  1 0                                            0.32                                                                               5  2 3  3 5  3 4 2  3 1  1  1 0                                            0.63                                                                               5  3 4  3 5  4 5 3  4 3  3  2 2                                         8-a                                                                               2.5 5  1 5  2 5  4 4 3  4 2  4  2 2                                         10-a                                                                              2.5 5  2 5  3 5  3 4 3  3 3  4  1 3                                         12-a                                                                              0.16                                                                               4  3 4  3 2  4 4 1  3 0  0  0 0                                            0.32                                                                               5  4 5  4 3  5 5 2  3 0  1  0 1                                            0.63                                                                               5  5 5  5 4  5 5 3  4 1  2  1 1                                         20-a                                                                              0.16                                                                               5  0 2  4 4  4 4 2  4 0  0  0 1                                            0.32                                                                               5  1 2  5 5  5 5 3  5 1  1  0 1                                            0.63                                                                               5  2 3  5 5  5 5 4  5 2  2  1 1                                         22-a                                                                              0.63                                                                               5  1 2  5 5  5 5 2  4 1  2  0 3                                         24-a                                                                              0.63                                                                               5  2 4  4 4  5 5 3  4 1  1  0 1                                         30-a                                                                              2.5 3  0 5  4 4  2 5 3  5 1  3  1 3                                         31-a                                                                              2.5 2  0 5  3 4  5 5 3  4 1  1  0 1                                         34-a                                                                              2.5 5  5 3  5 5  4 4 2  5 1  1  0 3                                         36-a                                                                              2.5 4  0 2  4 4  4 3 0  3 0  0  0 0                                         38-a                                                                              2.5 5  3 4  5 5  3 4 4  5 2  3  0 1                                         40-a                                                                              2.5 5  3 5  5 4  3 4 4  5 3  3  1 0                                         47-a                                                                              2.5 5  2 5  5 3  5 5 4  5 1  3  1 3                                         48-a                                                                              2.5 5  2 5  5 5  5 5 5  5 3  4  1 5                                         56-a                                                                              2.5 5  3 5  3 5  3 5 3  4 1  3  0 3                                         59-a                                                                              2.5 5  2 5  5 5  5 5 4  5 2  3  1 5                                         63-a                                                                              2.5 5  3 3  5 5  5 5 3  5 1  4  1 4                                         64-a                                                                              2.5 5  3 5  5 5  5 5 4  5 3  3  0 4                                         73-a                                                                              0.16                                                                               5  5 5  4 2  5 5 4  5 4  4  1 0                                         74-a                                                                              0.63                                                                               5  5 3  4 5  5 5 1  5 2  1  1 4                                         1-c                                                                               0.16                                                                               5  5 5  5 5  5 5 4  5 1  4  1 5                                         2-c                                                                               0.16                                                                               5  5 5  5 4  5 5 4  4 2  3  1 4                                         3-c                                                                               0.16                                                                               5  5 5  5 5  5 5 5  4 2  4  1 5                                         4-c                                                                               0.63                                                                               5  2 1  3 3  5 5 3  4 0  0  0 4                                         5-c                                                                               0.63                                                                               5  5 5  5 5  5 5 3  5 3  3  3 5                                         6-c                                                                               0.63                                                                               5  5 4  5 5  5 5 2  5 2  4  2 5                                         7-c                                                                               0.63                                                                               5  5 4  5 5  5 5 3  4 1  3  3 4                                         8-c                                                                               10  2  2 2  3 5  5 5 0  3 0  0  2 4                                         11-c                                                                              0.63                                                                               5  5 5  5 5  5 5 3  4 3  3  4 5                                         12-c                                                                              0.16                                                                               5  5 4  5 5  5 5 2  5 1  4  3 5                                         13-c                                                                              0.16                                                                               5  5 5  5 5  5 5 3  5 3  5  4 5                                         14-c                                                                              0.63                                                                               5  5 5  5 2  5 5 2  4 0  0  3 5                                         15-c                                                                              0.63                                                                               5  5 4  5 5  5 5 3  5 0  0  2 5                                         16-c                                                                              0.63                                                                               5  5 4  5 5  5 5 3  5 3  4  4 5                                         17-c                                                                              0.63                                                                               5  4 3  5 5  5 5 1  5 1  3  3 4                                         18-c                                                                              0.16                                                                               5  5 4  5 5  5 5 2  5 3  4  4 5                                         20-c                                                                              0.63                                                                               1  1 0  0 5  5 5 0  0 0  0  1 2                                         21-c                                                                              0.63                                                                               3  5 2  3 5  5 5 1  3 0  0  1 2                                         23-c                                                                              0.63                                                                               5  4 3  5 5  5 5 1  1 0  0  1 1                                         24-c                                                                              0.16                                                                               5  5 5  2 3  5 5 4  5 1  5  3 3                                         26-c                                                                              0.63                                                                               5  5 5  3 4  5 5 5  5 5  5  0 3                                         35-c                                                                              0.16                                                                               5  5 5  5 5  5 5 4  5 4  3  3 5                                         36-c                                                                              0.16                                                                               5  5 5  5 5  5 5 4  5 4  4  3 5                                         37-c                                                                              0.16                                                                               5  5 5  5 5  5 5 5  5 5  5  3 5                                         38-c                                                                              0.63                                                                               5  5 3  5 5  5 5 3  5 2  4  2 5                                         39-c                                                                              0.63                                                                               5  5 5  5 4  5 5 4  5 2  5  4 4                                         40-c                                                                              0.16                                                                               5  5 5  5 5  5 5 5  5 5  5  4 5                                         5-d                                                                               10  4  5 2  5 5  5 5 2  4 1  3  3 5                                         6-d                                                                               10  3  4 4  5 5  5 5 2  3 1  2  3 5                                         9-d                                                                               10  2  4 4  4 5  5 5 0  4 0  3  2 3                                         1-e                                                                               5   4  2 2  3 5  5 5 3  5 1  2  0 3                                         2-e                                                                               2.5 3  0 0  1 3  0 1 1  0 0  0  0 1                                         4-e                                                                               5   2  0 4  4 5  5 3 2  3 0  0  0 4                                         2-f                                                                               10  3  0 2  2 5  5 4 1  3 0  2  0 3                                         1-g                                                                               2.5 5  4 -- 5 5  5 5 4  4 2  4  1 4                                         7-g                                                                               2.5 2  3 5  5 5  5 5 1  5 2  4  3 5                                         9-g                                                                               2.5 2  3 4  5 5  4 5 0  3 1  5  2 5                                         11-g                                                                              2.5 5  5 3  5 5  5 5 2  5 4  4  3 4                                         12-g                                                                              2.5 4  3 3  3 5  5 5 0  4 1  4  1 3                                         13-g                                                                              2.5 4  2 3  3 5  5 5 0  4 1  4  1 3                                         14-g                                                                              2.5 3  1 3  3 5  5 5 0  4 1  4  1 3                                         15-g                                                                              2.5 4  3 5  5 5  5 5 1  5 3  4  2 4                                         16-g                                                                              2.5 5  3 5  5 5  5 5 2  5 3  5  2 4                                         17-g                                                                              2.5 5  5 5  4 5  5 5 5  5 5  5  1 3                                         18-g                                                                              2.5 5  5 5  4 5  5 5 5  5 5  5  3 5                                         19-g                                                                              2.5 3  2 2  3 5  5 3 1  4 2  3  2 3                                         __________________________________________________________________________

                  TABLE 17                                                         ______________________________________                                                Dose                                                                    No.    (kg/ha) A       H   I     J   K     L   a                               ______________________________________                                         74-a   2.5     5       4   4     4   5     4   0                               1-b    4       4       --  5     5   5     --  0                               1-c    0.64    5       5   4     5   5     5   0                               7-c    2.5     5       0   4     4   4     4   0                               13-c   0.64    5       4   5     4   5     5   0                               50-c   0.64    5       4   5     5   5     4   0                               53-c   0.16    5       0   4     5   4     2   0                               54-c   0.16    5       2   4     4   5     5   0                               ______________________________________                                    

TEST EXAMPLE 4

Test-2 on the herbicidal effects in soil treatment

A plastic box having a length of 21 cm, a width of 13 cm and a depth of 7 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Setaria viridis, Avena fatua, Alopecurus myosuroides, Abutilon theophrasti, Xanthium strumarium, Amaranthus viridis, Ipomoea spp., Veronica persica, Stellaria media, Zea mays, Oryza sativa, Oryza sativa, Glycine max, Gossypium spp., Triticum aestivum and Beta vulgaris were spot-wisely sown, and the soil was covered thereon in a thickness of about 1.5 cm, and then a herbicide solution was applied onto the surface of the soil uniformly so that the active ingredient was distributed at a predetermined concentration. The herbicide solution was prepared by diluting a wettable powder prepared in accordance with the foregoing Formulation Examples with water and applied onto the entire soil surface by a small spray. Three weeks after the application of the herbicidal solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were visually determined on the basis of the following standard ratings. The results are shown in Table 18.

Some of the compounds of the present invention show selectivity for certain crop plants.

Standard ratings:

5: Growth control rate of more than 90% (almost completely withered)

4: Growth control rate of from 70 to 90%

3: Growth control rate of from 40 to 70%

2: Growth control rate of from 20 to 40%

1: Growth control rate of from 5 to 20%

0: Growth control rate of less than 5% (almost non-effective)

TEST EXAMPLE 5

Test-2 on the herbicidal effects in foliage treatment

A plastic box having a length of 21 cm, a width of 13 cm and a depth of 7 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Setaria viridis, Avena fatua, Alopecurus myosuroides, Abutilon theophrasti, Xanthium strumarium, Amaranthus viridis, Ipomoea spp., Veronica persica, Stellaria media, Zea mays, Oryza sativa, Glycine max, Gossypium spp., Triticum aestivum and Beta Vulgaris were spot-wisely sown and the soil was covered thereon in a thickness of about 1.5 cm. When the various weeds and crop plants grew to the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient was applied in a predetermined concentration. The herbicidal solution was prepared by diluting a wettable powder prepared in accordance with the above Formulation Examples with water and applied onto the entire surface of the foliages of the weeds and the crop plants by a small spray. Three weeks after the application of the herbicide solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were visually determined on the basis of the standard ratings described in Test Example 4. The results are shown in Table 19.

TEST EXAMPLE 6

Test-2 on the herbicidal effects during the growing stage in irrigation treatment

Into a Wagner pot of 1/5000a, alluvial soil was put, and then water was introduced and mixed to form an irrigated state with a water depth of 4 cm. Seeds of Echinochloa crus-galli, Scirpus juncoides, Monochoria vaginalis and Rotala indica were sown in the above pot. The pot was placed in a greenhouse at a temperature of from 25° to 30° C., and the plants were cultured. When Echinochloa crus-galli, Scirpus juncoides, Monochoria vaginalis and Rotala indica reached 1 to 2 leaf stage, a diluted solution of the herbicide was dropwise applied to the water surface by a measuring pipette, so that the dose would be a predetermined level. Three weeks after the dropwise application of the herbicide, the herbicidal effects to various weeds were visually determined on the basis of the standard ratings described in Test Example 4. The results are shown in Table 20.

In Tables 18, 19 and 20, Nos. correspond to Compound Nos. in the Examples, and symbols have the following meanings.

A: Echinochloa crus-galli (barnyardgrass)

B: Setaria viridis (green foxtail)

C: Avena fatua (wild oat)

D: Alopecurus myosuroides (black grass)

E: Abutilon theophrasti (velvetleaf)

F: Xanthium strumarium (common cocklebur)

G: Amaranthus viridis (slender amaranth)

H: Ipomoea spp. (mornigglory)

I: Veronica persica (Persian speedwell)

J: Stellaria media (common chickweed)

K: Scirpus juncoides

L: Monochoria vaginalis

M: Rotala indica

a: Zea mays (corn)

b: Oryza sativa (rice)

c: Glycine max (soybean)

d: Gossypium spp. (cotton)

e: Triticum aestivum (wheat)

f: Beta vulgaris (sugar beet)

                                      TABLE 18                                     __________________________________________________________________________        Dose                                                                        No.                                                                               (kg/ha)                                                                            A B C D E F G H I J a b c d e f                                         __________________________________________________________________________     41-c                                                                              0.16                                                                               5 5 3 5 5 5 5 4 2 5 4 5 3 0 3 4                                         43-c                                                                              0.63                                                                               5 5 3 5 3 1 5 3 5 5 5 5 1 0 4 4                                         44-c                                                                              0.63                                                                               5 5 5 5 5 3 5 5 5 5 5 5 4 0 4 4                                         49-c                                                                              0.63                                                                               5 5 2 5 5 2 5 5 5 5 5 5 0 2 2 5                                         50-c                                                                              0.63                                                                               5 5 4 5 5 2 5 5 5 5 5 5 1 1 3 5                                         51-c                                                                              0.16                                                                               5 5 4 5 5 5 5 5 5 5 5 5 3 1 2 4                                         52-c                                                                              0.63                                                                               5 5 5 5 2 5 5 5 5 5 5 5 3 3 4 4                                         53-c                                                                              0.16                                                                               5 5 5 5 2 5 5 5 5 5 4 5 0 0 4 5                                         54-c                                                                              0.63                                                                               5 5 5 5 5 5 5 5 5 5 5 5 3 1 4 5                                         55-c                                                                              0.63                                                                               5 5 5 5 4 5 5 5 5 5 5 5 1 0 5 5                                         56-c                                                                              0.63                                                                               5 5 5 5 5 5 5 5 5 5 5 5 3 1 5 5                                         20-g                                                                              0.63                                                                               5 5 3 5 5 2 5 3 5 5 4 4 2 0 2 5                                         __________________________________________________________________________

                                      TABLE 19                                     __________________________________________________________________________        Dose                                                                        No.                                                                               (kg/ha)                                                                            A B C D E F G H I J a b c d e f                                         __________________________________________________________________________     41-c                                                                              0.16                                                                               5 5 4 5 5 5 5 5 1 5 5 3 4 2 2 5                                         43-c                                                                              0.63                                                                               5 5 4 5 5 5 5 3 2 5 5 3 0 1 2 5                                         44-c                                                                              0.63                                                                               5 5 5 5 5 5 5 5 3 5 5 4 4 3 3 5                                         49-c                                                                              0.63                                                                               5 5 2 5 5 5 5 5 5 5 5 2 4 2 1 5                                         50-c                                                                              0.63                                                                               5 5 3 5 5 5 5 5 4 5 5 3 4 3 1 5                                         51-c                                                                              0.16                                                                               5 5 3 4 5 5 5 5 5 5 5 4 5 1 2 5                                         52-c                                                                              0.63                                                                               5 5 5 5 5 5 5 4 2 5 5 4 4 1 4 5                                         53-c                                                                              0.16                                                                               5 5 5 5 5 5 5 5 5 5 5 5 5 3 4 5                                         54-c                                                                              0.16                                                                               5 5 5 5 5 5 5 5 5 5 5 5 5 3 3 5                                         55-c                                                                              0.16                                                                               5 5 5 5 5 5 5 3 5 5 5 5 5 1 5 5                                         56-c                                                                              0.16                                                                               5 5 5 5 5 5 5 2 5 5 5 5 5 1 5 5                                         20-g                                                                              0.63                                                                               5 5 5 5 5 5 5 4 5 5 5 5 5 3 4 5                                         __________________________________________________________________________

                  TABLE 20                                                         ______________________________________                                                 Dose                                                                   No.     (kg/ha)     A     K      L     M                                       ______________________________________                                         50-c    0.64        5     4      4     4                                       53-c    0.16        5     3      4     2                                       54-c    0.16        5     4      4     4                                       ______________________________________                                    

INDUSTRIAL APPLICABILITY

Iminosulfonylurea derivatives of the formula (1) of the present invention can be used safely to important crop plants, and they are compounds showing high herbicidal effects against many weeds and thus useful as active ingredients of herbicides. 

We claim:
 1. A compound of the formula: ##STR778## wherein Q is: ##STR779## each of R^(a1), R^(b1), R^(c1), R^(d1), R^(f1) are, independently, a C1-8 alkyl group; a C₃₋₇ cycloalkyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group; a C₃₋₇ cycloalkenyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or polyhalogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group; a mono-, di- or poly-halogeno C₂₋₈ alkenyl group; a mono-, di- or poly-halogen C₂₋₈ alkynyl group; a C₁₋₆ alkyl group substituted by a cyano group; a C₂₋₆ alkenyl group substituted by a cyano group; a C₂₋₆ alkynyl group substituted by a cyano group; a C₁₋₆ alkyl group substituted by a nitro group; a C₂₋₆ alkenyl group substituted by a nitro group; a C₂₋₆ alkynyl group substituted by a nitro group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group; a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group; a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group; a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group; a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group; a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group; a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group; a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group; a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group; a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group; a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group; a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group; a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group; a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group; a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₂₋₇ alkenyl group substituted by a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₂₋₆ alkynyl group substituted by a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a phenoxy group, provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a phenylthio group, provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a phenylsulfinyl group, provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a phenylsulfonyl group, provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a benzylthio group, provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a benzylsulfinyl group, provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a benzylsulfonyl group; a C₁₋₆ alkyl group substituted by a benzylsulfonyl group which is substituted on the phenyl group of the benzylsulfonyl group by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a phenylcarbonyl group; a C₁₋₆ alkyl group substituted by a phenylcarbonyl group wherein the phenylcarbonyl group is substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a benzylcarbonyl group; a C₁₋₆ alkyl group substituted by a benzylcarbonyl wherein the phenyl ring of the benzylcarbonyl group is substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group; or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,R^(b2) is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; each of R^(a4) and R^(a5) which are independent of each other, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; R^(a6) is C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group or a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group, consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; R^(b3) is a hydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group; each of R^(b4) and R^(b5) are, independently, a hydrogen atom or a C₁₋₆ alkyl group; each of R^(c2), R^(c3), R^(d2), R^(d3), R^(d4), R^(f5) and R^(f6) are, independently, a hydrogen atom, a C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a phenyl group or a phenyl group substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; R^(d5) a C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a phenyl group or a phenyl group substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; R^(d6) and R^(f2) are, independently, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcorbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy, and a C₂₋₇ alkoxycarbonyl group; or a C₁₋₆ alkyl group substituted by a phenyl group, provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; X is an oxygen atom or a sulfur atom, L is a hydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group, G is ##STR780## A is a nitrogen atom, and each of B and D are, independently, a C₁₋₄ alkyl group, a C₁₋₄ alkoxy group, a mono-, di- or poly-halogeno C₁₋₄ alkyl group, a mono-, di- or poly-halogeno C₁₋₄ alkoxy group, a halogen atom, a C₁₋₄ alkylamino group or a di(C₁₋₃ alkyl)amino group.
 2. The iminosulfonylurea derivative or its salt according to claim 1, wherein Q is ##STR781##
 3. The iminosulfonylurea derivative or its salt according to claim 1, wherein Q is ##STR782##
 4. The iminosulfonylurea derivative or its salt according to claim 1, wherein Q is ##STR783##
 5. The iminosulfonylurea derivative or its salt according to claim 1, wherein Q is ##STR784##
 6. The iminosulfonylurea derivative or its salt according to claim 1, wherein Q is ##STR785##
 7. A method of controlling the growth of weeds, comprising applying a herbicidally effective amount of a compound according to claim
 1. 8. A herbicidal composition, comprising a compound according to claim 1, and an inert carrier.
 9. A compound of the formula: ##STR786## where Q is: ##STR787## each of R^(a1), R^(c1), and R^(f1) are, independently, a C₁₋₈ alkyl group; a C₃₋₇ cycloalkyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group; a C₃₋₇ cycloalkenyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or polyhalogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group; a mono-, di- or poly-halogeno C₂₋₈ alkenyl group; a mono-, di- or poly-halogen C₂₋₈ alkynyl group; a C₁₋₆ alkyl group substituted by a cyano group; a C₂₋₆ alkenyl group substituted by a cyano group; a C₂₋₆ alkynyl group substituted by a cyano group; a C₁₋₆ alkyl group substituted by a nitro group; a C₂₋₆ alkenyl group substituted by a nitro group; a C₂₋₆ alkynyl group substituted by a nitro group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group; a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group; a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group; a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group; a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group; a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group; a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group; a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group; a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group; a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group; a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group; a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group; a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group; a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group; a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group; a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group; a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group; a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group; a C₁₋₆ alkyl group substituted by a benzylsulfonyl group which is substituted on the phenyl group of the benzylsulfonyl group by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a phenylcarbonyl group; a C₁₋₆ alkyl group substituted by a phenylcarbonyl group wherein the phenylcarbonyl group is substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by a benzylcarbonyl group; a C₁₋₆ alkyl group substituted by a benzylcarbonyl wherein the phenyl ring of the benzylcarbonyl group is substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group; a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group; or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,each of R^(a2), R^(a3), R^(c7), R^(c8), R^(f3) and R^(f4) are, independently, a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogen C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group); R^(a6) is C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group, consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), R^(f2) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl a group, C₁₋₆ alkoxy group, and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), X is an oxygen atom or a sulfur atom, L is a hydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group, G is ##STR788## A is a nitrogen atom, and each of B and D are, independently, a C₁₋₄ alkyl group, a C₁₋₄ alkoxy group, a mono-, di- or poly-halogeno C₁₋₄ alkyl group, a mono-, di- or poly-halogeno C₁₋₄ alkoxy group, a halogen atom, a C₁₋₄ alkylamino group or a di(C₁₋₃ alkyl)amino group.
 10. A method of controlling the growth of weeds, comprising applying a herbicidally effective amount of a compound according to claim
 9. 11. A herbicidal composition, comprising a compound according to claim 9, and an inert carrier. 